Chemicals

Showing 10351–10500 of 41137 results

  • Aurintricarboxylic acid (ATA) is an inhibitor of protein synthesis that has diverse biological activities.{54334,54335,54336,54337,54338,54339,54340,54341} It inhibits the activity of a variety of enzymes, including the nucleases DNase I, RNase A, and S1, as well as the serine proteases trypsin and chymotrypsin in a concentration-dependent manner.{54335,54336} ATA inhibits replication of severe acute respiratory syndrome coronavirus (SARS-CoV; EC50 = 200 µg/ml) and human enterovirus 71 in Vero cells (EV71; EC50 = 2.9 µM), as well as reduces HIV-1- or HIV-2-induced cytopathogenicity in MT-4 cells (IC50s = 1.1 and 0.85 µg/ml, respectively).{54337,54338,54339} It inhibits apoptosis induced by sanguinarine (Item No. 16951) in K562 leukemia cells when used at a concentration of 100 µM.{54340} ATA (20 mg/kg, i.p.) decreases CNS CD4+ T cell infiltration and reduces hind limb weakness and paralysis in a mouse model of myelin oligodendrocyte glycoprotein-induced experimental autoimmune encephalomyelitis (EAE).{54341}  

     

    Brand:
    Cayman
    SKU:30636 - 50 g

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  • Aurodox is a polyketide antibiotic originally isolated from S. goldiniensis.{42705} It is active against Gram-positive bacteria, including B. megaterium, B. anthracis, and M. hominis (MICs = 0.06, 0.6, and 3-10 µg/ml, respectively), as well as Pneumococcus and Streptomyces species (MICs = 3-12 and 3-30 µg/ml, respectively). It is effective against S. pyogenes infection in mice with a 50% curative dose (CD50) value of 71 mg/kg. Aurodox inhibits bacterial protein synthesis by binding to bacterial elongation factor Tu (EF-Tu) and inhibiting its release from the ribosome.{42706,42707}  

     

    Brand:
    Cayman
    SKU:27584 - 1 mg

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  • Aurodox is a polyketide antibiotic originally isolated from S. goldiniensis.{42705} It is active against Gram-positive bacteria, including B. megaterium, B. anthracis, and M. hominis (MICs = 0.06, 0.6, and 3-10 µg/ml, respectively), as well as Pneumococcus and Streptomyces species (MICs = 3-12 and 3-30 µg/ml, respectively). It is effective against S. pyogenes infection in mice with a 50% curative dose (CD50) value of 71 mg/kg. Aurodox inhibits bacterial protein synthesis by binding to bacterial elongation factor Tu (EF-Tu) and inhibiting its release from the ribosome.{42706,42707}  

     

    Brand:
    Cayman
    SKU:27584 - 5 mg

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  • Aurodox is a polyketide antibiotic originally isolated from S. goldiniensis.{42705} It is active against Gram-positive bacteria, including B. megaterium, B. anthracis, and M. hominis (MICs = 0.06, 0.6, and 3-10 µg/ml, respectively), as well as Pneumococcus and Streptomyces species (MICs = 3-12 and 3-30 µg/ml, respectively). It is effective against S. pyogenes infection in mice with a 50% curative dose (CD50) value of 71 mg/kg. Aurodox inhibits bacterial protein synthesis by binding to bacterial elongation factor Tu (EF-Tu) and inhibiting its release from the ribosome.{42706,42707}  

     

    Brand:
    Cayman
    SKU:27584 - 500 µg

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  • Aurora A inhibitor I is a potent and selective inhibitor of Aurora A kinase (IC50s = 3.4 and 3,400 nM for Aurora A and Aurora B, respectively).{38453} It prevents centrosome separation and reduces phosphorylated Aurora A, but not phosphorylated histone H3, levels at the centrosomes, indicating inhibition is specific to Aurora A kinase. Aurora A inhibitor I reduces the proliferation of HCT116 and HT-29 colorectal carcinoma cells in vitro (IC50s = 0.19 and 2.9 μM, respectively).  

     

    Brand:
    Cayman
    SKU:21600 -

    Out of stock

  • Aurora A inhibitor I is a potent and selective inhibitor of Aurora A kinase (IC50s = 3.4 and 3,400 nM for Aurora A and Aurora B, respectively).{38453} It prevents centrosome separation and reduces phosphorylated Aurora A, but not phosphorylated histone H3, levels at the centrosomes, indicating inhibition is specific to Aurora A kinase. Aurora A inhibitor I reduces the proliferation of HCT116 and HT-29 colorectal carcinoma cells in vitro (IC50s = 0.19 and 2.9 μM, respectively).  

     

    Brand:
    Cayman
    SKU:21600 -

    Out of stock

  • Aurora A inhibitor I is a potent and selective inhibitor of Aurora A kinase (IC50s = 3.4 and 3,400 nM for Aurora A and Aurora B, respectively).{38453} It prevents centrosome separation and reduces phosphorylated Aurora A, but not phosphorylated histone H3, levels at the centrosomes, indicating inhibition is specific to Aurora A kinase. Aurora A inhibitor I reduces the proliferation of HCT116 and HT-29 colorectal carcinoma cells in vitro (IC50s = 0.19 and 2.9 μM, respectively).  

     

    Brand:
    Cayman
    SKU:21600 -

    Out of stock

  • Aurora A inhibitor I is a potent and selective inhibitor of Aurora A kinase (IC50s = 3.4 and 3,400 nM for Aurora A and Aurora B, respectively).{38453} It prevents centrosome separation and reduces phosphorylated Aurora A, but not phosphorylated histone H3, levels at the centrosomes, indicating inhibition is specific to Aurora A kinase. Aurora A inhibitor I reduces the proliferation of HCT116 and HT-29 colorectal carcinoma cells in vitro (IC50s = 0.19 and 2.9 μM, respectively).  

     

    Brand:
    Cayman
    SKU:21600 -

    Out of stock

  • The Aurora kinases are a family of serine/threonine kinases that are key regulators of mitosis and cytokinesis. Aurora kinase inhibitor II is a cell-permeable anilinoquinazoline that blocks the activity of Aurora A (IC50 = 0.39 µM).{29266} In MCF-7 cells, it blocks proliferation with an IC50 value of 1.25 µM.{29266}  

     

    Brand:
    Cayman
    SKU:-

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  • The Aurora kinases are a family of serine/threonine kinases that are key regulators of mitosis and cytokinesis. Aurora kinase inhibitor II is a cell-permeable anilinoquinazoline that blocks the activity of Aurora A (IC50 = 0.39 µM).{29266} In MCF-7 cells, it blocks proliferation with an IC50 value of 1.25 µM.{29266}  

     

    Brand:
    Cayman
    SKU:-

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  • The Aurora kinases are a family of serine/threonine kinases that are key regulators of mitosis and cytokinesis. Aurora kinase inhibitor II is a cell-permeable anilinoquinazoline that blocks the activity of Aurora A (IC50 = 0.39 µM).{29266} In MCF-7 cells, it blocks proliferation with an IC50 value of 1.25 µM.{29266}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • The Aurora kinases are a family of serine/threonine kinases that are key regulators of mitosis and cytokinesis. Aurora kinase inhibitor II is a cell-permeable anilinoquinazoline that blocks the activity of Aurora A (IC50 = 0.39 µM).{29266} In MCF-7 cells, it blocks proliferation with an IC50 value of 1.25 µM.{29266}  

     

    Brand:
    Cayman
    SKU:-

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  • Aurora kinase inhibitor III is a potent inhibitor of Aurora A kinase (IC50 = 42 nM).{25289} It is selective for Aurora A over BMX, BTK, IGF-1R, c-Src, TRKB, SYK, and EGFR (IC50s = 386, 3,550, 591, 1,980, 2,510, 887, and >10,000 nM, respectively).  

     

    Brand:
    Cayman
    SKU:21851 -

    Out of stock

  • Aurora kinase inhibitor III is a potent inhibitor of Aurora A kinase (IC50 = 42 nM).{25289} It is selective for Aurora A over BMX, BTK, IGF-1R, c-Src, TRKB, SYK, and EGFR (IC50s = 386, 3,550, 591, 1,980, 2,510, 887, and >10,000 nM, respectively).  

     

    Brand:
    Cayman
    SKU:21851 -

    Out of stock

  • Aurora kinase inhibitor III is a potent inhibitor of Aurora A kinase (IC50 = 42 nM).{25289} It is selective for Aurora A over BMX, BTK, IGF-1R, c-Src, TRKB, SYK, and EGFR (IC50s = 386, 3,550, 591, 1,980, 2,510, 887, and >10,000 nM, respectively).  

     

    Brand:
    Cayman
    SKU:21851 -

    Out of stock

  • Australine is a pyrrolizidine alkaloid originally isolated from C. australe that has enzyme inhibitory activities.{54015,54016,54017} It is an inhibitor of glucoamylase (IC50 = 5.8 µM) that also inhibits glucosidase I, sucrase, maltase, and A. niger α-glucosidase (IC50s = 20, 28, 35, and 28 µM, respectively).{54016,54017} Australine is selective for these enzymes over glucosidase II, α- and β-mannosidase, and α- and β-galactosidase up to 500 µM, β-glucosidase, with only 5% inhibition at 66 µM, as well as isomaltase and trehalase (IC50 = 97 and 160 µM, respectively). Australine (500 µg/ml) inhibits glycoprotein processing of viral glycoproteins in influenza virus-infected MDCK cells and induces the accumulation of glycoproteins.{54016}  

     

    Brand:
    Cayman
    SKU:30051 - 1 mg

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  • Australine is a pyrrolizidine alkaloid originally isolated from C. australe that has enzyme inhibitory activities.{54015,54016,54017} It is an inhibitor of glucoamylase (IC50 = 5.8 µM) that also inhibits glucosidase I, sucrase, maltase, and A. niger α-glucosidase (IC50s = 20, 28, 35, and 28 µM, respectively).{54016,54017} Australine is selective for these enzymes over glucosidase II, α- and β-mannosidase, and α- and β-galactosidase up to 500 µM, β-glucosidase, with only 5% inhibition at 66 µM, as well as isomaltase and trehalase (IC50 = 97 and 160 µM, respectively). Australine (500 µg/ml) inhibits glycoprotein processing of viral glycoproteins in influenza virus-infected MDCK cells and induces the accumulation of glycoproteins.{54016}  

     

    Brand:
    Cayman
    SKU:30051 - 500 µg

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  • AUT1 is a positive modulator of the voltage-gated potassium channel subtypes Kv3.1b, Kv3.2a, and Kv3.3 (EC50s = 4.7, 4.9, and 31.6 µM, respectively, in a patch-clamp assay).{46494} It is selective for Kv3.1b, Kv3.2a, and Kv3.3 over Kv1.5 and Kv7.1/minK channels but also inhibits the serotonin (5-HT) transporter, 5-HT3 receptor, and α1 subunit-containing nicotinic acetylcholine receptor (nAChR) in a panel of 26 ion channels, receptors, and transporters. AUT1 increases tetraethylammonium-induced decreases in the firing frequency and amplitude of action potentials in mouse somatosensory cortex slices when used at concentrations of 1 and 10 µM.  

     

    Brand:
    Cayman
    SKU:28599 - 10 mg

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  • AUT1 is a positive modulator of the voltage-gated potassium channel subtypes Kv3.1b, Kv3.2a, and Kv3.3 (EC50s = 4.7, 4.9, and 31.6 µM, respectively, in a patch-clamp assay).{46494} It is selective for Kv3.1b, Kv3.2a, and Kv3.3 over Kv1.5 and Kv7.1/minK channels but also inhibits the serotonin (5-HT) transporter, 5-HT3 receptor, and α1 subunit-containing nicotinic acetylcholine receptor (nAChR) in a panel of 26 ion channels, receptors, and transporters. AUT1 increases tetraethylammonium-induced decreases in the firing frequency and amplitude of action potentials in mouse somatosensory cortex slices when used at concentrations of 1 and 10 µM.  

     

    Brand:
    Cayman
    SKU:28599 - 100 mg

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  • AUT1 is a positive modulator of the voltage-gated potassium channel subtypes Kv3.1b, Kv3.2a, and Kv3.3 (EC50s = 4.7, 4.9, and 31.6 µM, respectively, in a patch-clamp assay).{46494} It is selective for Kv3.1b, Kv3.2a, and Kv3.3 over Kv1.5 and Kv7.1/minK channels but also inhibits the serotonin (5-HT) transporter, 5-HT3 receptor, and α1 subunit-containing nicotinic acetylcholine receptor (nAChR) in a panel of 26 ion channels, receptors, and transporters. AUT1 increases tetraethylammonium-induced decreases in the firing frequency and amplitude of action potentials in mouse somatosensory cortex slices when used at concentrations of 1 and 10 µM.  

     

    Brand:
    Cayman
    SKU:28599 - 50 mg

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  • AUTEN-99 is an inhibitor of the phosphatase myotubularin-related protein 14 (MTMR14/Jumpy).{53584} It inhibits MTMR14/Jumpy activity in a cell-free assay when used at concentrations of 10 and 100 µM. AUTEN-99 (1 and 10 µM) enhances autophagic flux and increases the levels of LC3B-11 in HeLa cells. It increases survival of mouse primary neurons exposed to hydrogen peroxide as a model of oxidative stress when used at concentrations ranging from 0.5 to 5 µM. AUTEN-99 increases the number of autophagic structures in mouse pancreas, kidney, and liver following oral or intraperitoneal administration. It also induces autophagy in the Drosophila larval fat body and increases the percentage of flies climbing a glass column in a climbing assay in a transgenic model of Parkinson’s disease.  

     

    Brand:
    Cayman
    SKU:30047 - 1 mg

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  • AUTEN-99 is an inhibitor of the phosphatase myotubularin-related protein 14 (MTMR14/Jumpy).{53584} It inhibits MTMR14/Jumpy activity in a cell-free assay when used at concentrations of 10 and 100 µM. AUTEN-99 (1 and 10 µM) enhances autophagic flux and increases the levels of LC3B-11 in HeLa cells. It increases survival of mouse primary neurons exposed to hydrogen peroxide as a model of oxidative stress when used at concentrations ranging from 0.5 to 5 µM. AUTEN-99 increases the number of autophagic structures in mouse pancreas, kidney, and liver following oral or intraperitoneal administration. It also induces autophagy in the Drosophila larval fat body and increases the percentage of flies climbing a glass column in a climbing assay in a transgenic model of Parkinson’s disease.  

     

    Brand:
    Cayman
    SKU:30047 - 10 mg

    Available on backorder

  • AUTEN-99 is an inhibitor of the phosphatase myotubularin-related protein 14 (MTMR14/Jumpy).{53584} It inhibits MTMR14/Jumpy activity in a cell-free assay when used at concentrations of 10 and 100 µM. AUTEN-99 (1 and 10 µM) enhances autophagic flux and increases the levels of LC3B-11 in HeLa cells. It increases survival of mouse primary neurons exposed to hydrogen peroxide as a model of oxidative stress when used at concentrations ranging from 0.5 to 5 µM. AUTEN-99 increases the number of autophagic structures in mouse pancreas, kidney, and liver following oral or intraperitoneal administration. It also induces autophagy in the Drosophila larval fat body and increases the percentage of flies climbing a glass column in a climbing assay in a transgenic model of Parkinson’s disease.  

     

    Brand:
    Cayman
    SKU:30047 - 25 mg

    Available on backorder

  • AUTEN-99 is an inhibitor of the phosphatase myotubularin-related protein 14 (MTMR14/Jumpy).{53584} It inhibits MTMR14/Jumpy activity in a cell-free assay when used at concentrations of 10 and 100 µM. AUTEN-99 (1 and 10 µM) enhances autophagic flux and increases the levels of LC3B-11 in HeLa cells. It increases survival of mouse primary neurons exposed to hydrogen peroxide as a model of oxidative stress when used at concentrations ranging from 0.5 to 5 µM. AUTEN-99 increases the number of autophagic structures in mouse pancreas, kidney, and liver following oral or intraperitoneal administration. It also induces autophagy in the Drosophila larval fat body and increases the percentage of flies climbing a glass column in a climbing assay in a transgenic model of Parkinson’s disease.  

     

    Brand:
    Cayman
    SKU:30047 - 5 mg

    Available on backorder

  • Cyclic Enzymatic method for the determination of 3-Hydroxybutyrate in serum or plasma.

    Brand:
    FUJIFILM Medical Systems USA
    SKU:413-73601

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  • The Autokit Glucose uses enzymatic method the determination of glucose in serum, plasma, and urine.

    Brand:
    FUJIFILM Medical Systems USA
    SKU:997-03001

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  • Autokit Micro albumin uses turbidimetric Immunoassay method for the determination of urine albumin.

    Brand:
    FUJIFILM Medical Systems USA
    SKU:999-06001

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  • Used with Autokit Micro albumin catalog no. 999-06001

    Brand:
    FUJIFILM Medical Systems USA
    SKU:991-06201

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  • Autophinib is an ATP-competitive inhibitor of the PI3K VPS34 (IC50 = 19 nM).{49061} It inhibits autophagy induced by the mTOR inhibitor rapamycin (Item No. 13346) or by amino acid starvation (IC50s = 40 and 90 nM, respectively) in MCF-7 cells. Autophinib also induces apoptosis in amino acid-starved MCF-7 cells with an EC50 value of 234 nM.  

     

    Brand:
    Cayman
    SKU:27320 - 1 mg

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  • Autophinib is an ATP-competitive inhibitor of the PI3K VPS34 (IC50 = 19 nM).{49061} It inhibits autophagy induced by the mTOR inhibitor rapamycin (Item No. 13346) or by amino acid starvation (IC50s = 40 and 90 nM, respectively) in MCF-7 cells. Autophinib also induces apoptosis in amino acid-starved MCF-7 cells with an EC50 value of 234 nM.  

     

    Brand:
    Cayman
    SKU:27320 - 10 mg

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  • Autophinib is an ATP-competitive inhibitor of the PI3K VPS34 (IC50 = 19 nM).{49061} It inhibits autophagy induced by the mTOR inhibitor rapamycin (Item No. 13346) or by amino acid starvation (IC50s = 40 and 90 nM, respectively) in MCF-7 cells. Autophinib also induces apoptosis in amino acid-starved MCF-7 cells with an EC50 value of 234 nM.  

     

    Brand:
    Cayman
    SKU:27320 - 25 mg

    Available on backorder

  • Autophinib is an ATP-competitive inhibitor of the PI3K VPS34 (IC50 = 19 nM).{49061} It inhibits autophagy induced by the mTOR inhibitor rapamycin (Item No. 13346) or by amino acid starvation (IC50s = 40 and 90 nM, respectively) in MCF-7 cells. Autophinib also induces apoptosis in amino acid-starved MCF-7 cells with an EC50 value of 234 nM.  

     

    Brand:
    Cayman
    SKU:27320 - 5 mg

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  • AUY954 is an orally bioavailable and selective agonist of the sphingosine-1-phosphate receptor 1 (S1P1; EC50 = 1.2 nM for stimulating GTPγS binding to S1P1 in CHO cells).{14536} It is highly selective for the S1P1 receptor with EC50 values of >10,000, 1,210, >1,000, and 340 nM for S1P2, S1P3, S1P4, and S1P5 receptors, respectively. AUY954 reduces circulating lymphocytes and prevents rejection of rat heart allografts. In a rat model of experimental autoimmune neuritis, chronic treatment with AUY954 (10 mg/kg), starting on the day of immunization, almost completely prevents peripheral paralysis.{37100} In the same model, it also decreases T cell, B cell, and macrophage infiltration and perivascular demyelination in sciatic nerves.  

     

    Brand:
    Cayman
    SKU:9000548 - 1 mg

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  • AUY954 is an orally bioavailable and selective agonist of the sphingosine-1-phosphate receptor 1 (S1P1; EC50 = 1.2 nM for stimulating GTPγS binding to S1P1 in CHO cells).{14536} It is highly selective for the S1P1 receptor with EC50 values of >10,000, 1,210, >1,000, and 340 nM for S1P2, S1P3, S1P4, and S1P5 receptors, respectively. AUY954 reduces circulating lymphocytes and prevents rejection of rat heart allografts. In a rat model of experimental autoimmune neuritis, chronic treatment with AUY954 (10 mg/kg), starting on the day of immunization, almost completely prevents peripheral paralysis.{37100} In the same model, it also decreases T cell, B cell, and macrophage infiltration and perivascular demyelination in sciatic nerves.  

     

    Brand:
    Cayman
    SKU:9000548 - 5 mg

    Available on backorder

  • AUY954 is an orally bioavailable and selective agonist of the sphingosine-1-phosphate receptor 1 (S1P1; EC50 = 1.2 nM for stimulating GTPγS binding to S1P1 in CHO cells).{14536} It is highly selective for the S1P1 receptor with EC50 values of >10,000, 1,210, >1,000, and 340 nM for S1P2, S1P3, S1P4, and S1P5 receptors, respectively. AUY954 reduces circulating lymphocytes and prevents rejection of rat heart allografts. In a rat model of experimental autoimmune neuritis, chronic treatment with AUY954 (10 mg/kg), starting on the day of immunization, almost completely prevents peripheral paralysis.{37100} In the same model, it also decreases T cell, B cell, and macrophage infiltration and perivascular demyelination in sciatic nerves.  

     

    Brand:
    Cayman
    SKU:9000548 - 500 µg

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  • AV-412 is a dual inhibitor of EGFR and HER2 (IC50s = 1.4, 0.51, 0.79, 2.3, and 19 nM for the EGFR, EGFRL858R, EGFRT790M, EGFRL858R,T790M, and HER2 recombinant intracellular kinase domains, respectively).{46529} It is selective for EGFR and HER2 over IRK, MEK1, PKA, and PKC (IC50s = >10 μM) but also inhibits Abl, FLT1, and Src (IC50s = 41, 920, and 2,000 nM, respectively). AV-412 (10 and 30 μM) induces ubiquitination and degradation of HER2 in SK-BR-3 cells.{46530} It decreases levels of HER2 and estrogen receptor α (ERα) and increases levels of Hsp70 in MCF-7 cells when used at a concentration of 10 μM. AV-412 inhibits EGF-stimulated growth of A431 cells (IC50 = 0.1 μM).{46529} It reduces tumor growth in an A431 mouse xenograft model when administered at doses of 10 and 30 mg/kg and in a BT-474 mouse xenograft model at 30 mg/kg.  

     

    Brand:
    Cayman
    SKU:29039 - 10 mg

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  • AV-412 is a dual inhibitor of EGFR and HER2 (IC50s = 1.4, 0.51, 0.79, 2.3, and 19 nM for the EGFR, EGFRL858R, EGFRT790M, EGFRL858R,T790M, and HER2 recombinant intracellular kinase domains, respectively).{46529} It is selective for EGFR and HER2 over IRK, MEK1, PKA, and PKC (IC50s = >10 μM) but also inhibits Abl, FLT1, and Src (IC50s = 41, 920, and 2,000 nM, respectively). AV-412 (10 and 30 μM) induces ubiquitination and degradation of HER2 in SK-BR-3 cells.{46530} It decreases levels of HER2 and estrogen receptor α (ERα) and increases levels of Hsp70 in MCF-7 cells when used at a concentration of 10 μM. AV-412 inhibits EGF-stimulated growth of A431 cells (IC50 = 0.1 μM).{46529} It reduces tumor growth in an A431 mouse xenograft model when administered at doses of 10 and 30 mg/kg and in a BT-474 mouse xenograft model at 30 mg/kg.  

     

    Brand:
    Cayman
    SKU:29039 - 25 mg

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  • AV-412 is a dual inhibitor of EGFR and HER2 (IC50s = 1.4, 0.51, 0.79, 2.3, and 19 nM for the EGFR, EGFRL858R, EGFRT790M, EGFRL858R,T790M, and HER2 recombinant intracellular kinase domains, respectively).{46529} It is selective for EGFR and HER2 over IRK, MEK1, PKA, and PKC (IC50s = >10 μM) but also inhibits Abl, FLT1, and Src (IC50s = 41, 920, and 2,000 nM, respectively). AV-412 (10 and 30 μM) induces ubiquitination and degradation of HER2 in SK-BR-3 cells.{46530} It decreases levels of HER2 and estrogen receptor α (ERα) and increases levels of Hsp70 in MCF-7 cells when used at a concentration of 10 μM. AV-412 inhibits EGF-stimulated growth of A431 cells (IC50 = 0.1 μM).{46529} It reduces tumor growth in an A431 mouse xenograft model when administered at doses of 10 and 30 mg/kg and in a BT-474 mouse xenograft model at 30 mg/kg.  

     

    Brand:
    Cayman
    SKU:29039 - 5 mg

    Available on backorder

  • AV-412 is a dual inhibitor of EGFR and HER2 (IC50s = 1.4, 0.51, 0.79, 2.3, and 19 nM for the EGFR, EGFRL858R, EGFRT790M, EGFRL858R,T790M, and HER2 recombinant intracellular kinase domains, respectively).{46529} It is selective for EGFR and HER2 over IRK, MEK1, PKA, and PKC (IC50s = >10 μM) but also inhibits Abl, FLT1, and Src (IC50s = 41, 920, and 2,000 nM, respectively). AV-412 (10 and 30 μM) induces ubiquitination and degradation of HER2 in SK-BR-3 cells.{46530} It decreases levels of HER2 and estrogen receptor α (ERα) and increases levels of Hsp70 in MCF-7 cells when used at a concentration of 10 μM. AV-412 inhibits EGF-stimulated growth of A431 cells (IC50 = 0.1 μM).{46529} It reduces tumor growth in an A431 mouse xenograft model when administered at doses of 10 and 30 mg/kg and in a BT-474 mouse xenograft model at 30 mg/kg.  

     

    Brand:
    Cayman
    SKU:29039 - 50 mg

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  • γ-Secretase is a protease complex that cleaves single-pass transmembrane proteins, such as Notch receptors and β-amyloid precursor protein (APP), within the transmembrane domain.{27051,25415} Avagacestat is a potent, orally bioavailable inhibitor of γ-secretase that more potently inhibits the cleavage of APP to Aβ40 than signaling through Notch (IC50s = 0.30 and 58 nM, respectively).{27425} It shows good pharmacokinetics in rats, dogs, and humans and passes the blood-brain barrier, reducing plasma, brain, and cerebrospinal fluid Aβ40 levels.{27425,27428} While suppressing the production of Aβ38, Aβ40, and Aβ42, γ-secretase inhibitors, including avagacestat, increase the level of APP β-C-terminal fragment, both in vitro and in vivo, altering cell function.{27426} Avagacestat may impact Notch signaling in vivo, although it is generally considered a “Notch-sparing” γ-secretase inhibitor.{27427}  

     

    Brand:
    Cayman
    SKU:-

    Out of stock

  • γ-Secretase is a protease complex that cleaves single-pass transmembrane proteins, such as Notch receptors and β-amyloid precursor protein (APP), within the transmembrane domain.{27051,25415} Avagacestat is a potent, orally bioavailable inhibitor of γ-secretase that more potently inhibits the cleavage of APP to Aβ40 than signaling through Notch (IC50s = 0.30 and 58 nM, respectively).{27425} It shows good pharmacokinetics in rats, dogs, and humans and passes the blood-brain barrier, reducing plasma, brain, and cerebrospinal fluid Aβ40 levels.{27425,27428} While suppressing the production of Aβ38, Aβ40, and Aβ42, γ-secretase inhibitors, including avagacestat, increase the level of APP β-C-terminal fragment, both in vitro and in vivo, altering cell function.{27426} Avagacestat may impact Notch signaling in vivo, although it is generally considered a “Notch-sparing” γ-secretase inhibitor.{27427}  

     

    Brand:
    Cayman
    SKU:-

    Out of stock

  • γ-Secretase is a protease complex that cleaves single-pass transmembrane proteins, such as Notch receptors and β-amyloid precursor protein (APP), within the transmembrane domain.{27051,25415} Avagacestat is a potent, orally bioavailable inhibitor of γ-secretase that more potently inhibits the cleavage of APP to Aβ40 than signaling through Notch (IC50s = 0.30 and 58 nM, respectively).{27425} It shows good pharmacokinetics in rats, dogs, and humans and passes the blood-brain barrier, reducing plasma, brain, and cerebrospinal fluid Aβ40 levels.{27425,27428} While suppressing the production of Aβ38, Aβ40, and Aβ42, γ-secretase inhibitors, including avagacestat, increase the level of APP β-C-terminal fragment, both in vitro and in vivo, altering cell function.{27426} Avagacestat may impact Notch signaling in vivo, although it is generally considered a “Notch-sparing” γ-secretase inhibitor.{27427}  

     

    Brand:
    Cayman
    SKU:-

    Out of stock

  • Avanafil is an orally bioavailable, potent, and competitive inhibitor of phosphodiesterase (PDE) 5 (IC50 = 2.2 nM).{40239} It is selective, with IC50 values of 630, >5,000, and >5,000 nM for PDE6, PDE1-4, and PDE7-11, respectively, in an enzyme assay. Avanafil potentiates penile tumescence in dogs in a dose-dependent manner. Formulations containing avanafil have been used to treat erectile dysfunction.{40271}  

     

    Brand:
    Cayman
    SKU:23024 - 1 g

    Available on backorder

  • Avanafil is an orally bioavailable, potent, and competitive inhibitor of phosphodiesterase (PDE) 5 (IC50 = 2.2 nM).{40239} It is selective, with IC50 values of 630, >5,000, and >5,000 nM for PDE6, PDE1-4, and PDE7-11, respectively, in an enzyme assay. Avanafil potentiates penile tumescence in dogs in a dose-dependent manner. Formulations containing avanafil have been used to treat erectile dysfunction.{40271}  

     

    Brand:
    Cayman
    SKU:23024 - 100 mg

    Available on backorder

  • Avanafil is an orally bioavailable, potent, and competitive inhibitor of phosphodiesterase (PDE) 5 (IC50 = 2.2 nM).{40239} It is selective, with IC50 values of 630, >5,000, and >5,000 nM for PDE6, PDE1-4, and PDE7-11, respectively, in an enzyme assay. Avanafil potentiates penile tumescence in dogs in a dose-dependent manner. Formulations containing avanafil have been used to treat erectile dysfunction.{40271}  

     

    Brand:
    Cayman
    SKU:23024 - 250 mg

    Available on backorder

  • Avanafil is an orally bioavailable, potent, and competitive inhibitor of phosphodiesterase (PDE) 5 (IC50 = 2.2 nM).{40239} It is selective, with IC50 values of 630, >5,000, and >5,000 nM for PDE6, PDE1-4, and PDE7-11, respectively, in an enzyme assay. Avanafil potentiates penile tumescence in dogs in a dose-dependent manner. Formulations containing avanafil have been used to treat erectile dysfunction.{40271}  

     

    Brand:
    Cayman
    SKU:23024 - 500 mg

    Available on backorder

  • Acyl-Coenzyme A:cholesterol acyltransferases (ACAT1 and ACAT2) catalyze the formation of cholesterol esters from cholesterol and long chain fatty acyl-coenzyme A, and may play a role in the development of atherosclerosis.{20948} Avasimibe is an orally bioavailable inhibitor of ACAT (IC50s = 24 and 9.2 µM for ACAT1 and ACAT2, respectively).{21762} It reduces foam cell formation in human macrophages in vitro, enhancing free cholesterol efflux and inhibiting the uptake of modified LDL and dose-dependently reduces plasma total triglyceride and VLDL cholesterol levels in cholesterol-fed animal models.{29393,29394} Avasimibe inhibition of ACAT has been used to decrease amyloid β generation in models of Alzheimer’s disease.{29395}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • Acyl-Coenzyme A:cholesterol acyltransferases (ACAT1 and ACAT2) catalyze the formation of cholesterol esters from cholesterol and long chain fatty acyl-coenzyme A, and may play a role in the development of atherosclerosis.{20948} Avasimibe is an orally bioavailable inhibitor of ACAT (IC50s = 24 and 9.2 µM for ACAT1 and ACAT2, respectively).{21762} It reduces foam cell formation in human macrophages in vitro, enhancing free cholesterol efflux and inhibiting the uptake of modified LDL and dose-dependently reduces plasma total triglyceride and VLDL cholesterol levels in cholesterol-fed animal models.{29393,29394} Avasimibe inhibition of ACAT has been used to decrease amyloid β generation in models of Alzheimer’s disease.{29395}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • Acyl-Coenzyme A:cholesterol acyltransferases (ACAT1 and ACAT2) catalyze the formation of cholesterol esters from cholesterol and long chain fatty acyl-coenzyme A, and may play a role in the development of atherosclerosis.{20948} Avasimibe is an orally bioavailable inhibitor of ACAT (IC50s = 24 and 9.2 µM for ACAT1 and ACAT2, respectively).{21762} It reduces foam cell formation in human macrophages in vitro, enhancing free cholesterol efflux and inhibiting the uptake of modified LDL and dose-dependently reduces plasma total triglyceride and VLDL cholesterol levels in cholesterol-fed animal models.{29393,29394} Avasimibe inhibition of ACAT has been used to decrease amyloid β generation in models of Alzheimer’s disease.{29395}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • Acyl-Coenzyme A:cholesterol acyltransferases (ACAT1 and ACAT2) catalyze the formation of cholesterol esters from cholesterol and long chain fatty acyl-coenzyme A, and may play a role in the development of atherosclerosis.{20948} Avasimibe is an orally bioavailable inhibitor of ACAT (IC50s = 24 and 9.2 µM for ACAT1 and ACAT2, respectively).{21762} It reduces foam cell formation in human macrophages in vitro, enhancing free cholesterol efflux and inhibiting the uptake of modified LDL and dose-dependently reduces plasma total triglyceride and VLDL cholesterol levels in cholesterol-fed animal models.{29393,29394} Avasimibe inhibition of ACAT has been used to decrease amyloid β generation in models of Alzheimer’s disease.{29395}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • The central cannabinoid (CB1) receptor is a G protein-coupled receptor that is widely distributed in the central nervous system and several peripheral tissues and binds the active component of cannabis, Δ9-tetrahydrocannabinol.{6749} Signaling through the CB1 receptor is implicated in attentional and working memory deficits as well as obesity.{12559,14939,15542} AVE-1625 is a highly potent, selective antagonist for the CB1 receptor with Ki values of 0.16-0.44 nM.{15542} At 1-3 mg/kg, AVE-1625 significantly improves the performance of rodents in working memory tasks.{15542} At 30 mg/kg, AVE-1625 reduces caloric intake by more than 50% of controls and significantly increases lipolysis from fat tissues and reduces hepatic glycogen levels in rodents.{15541}  

     

    Brand:
    Cayman
    SKU:10009021 - 1 mg

    Available on backorder

  • The central cannabinoid (CB1) receptor is a G protein-coupled receptor that is widely distributed in the central nervous system and several peripheral tissues and binds the active component of cannabis, Δ9-tetrahydrocannabinol.{6749} Signaling through the CB1 receptor is implicated in attentional and working memory deficits as well as obesity.{12559,14939,15542} AVE-1625 is a highly potent, selective antagonist for the CB1 receptor with Ki values of 0.16-0.44 nM.{15542} At 1-3 mg/kg, AVE-1625 significantly improves the performance of rodents in working memory tasks.{15542} At 30 mg/kg, AVE-1625 reduces caloric intake by more than 50% of controls and significantly increases lipolysis from fat tissues and reduces hepatic glycogen levels in rodents.{15541}  

     

    Brand:
    Cayman
    SKU:10009021 - 10 mg

    Available on backorder

  • The central cannabinoid (CB1) receptor is a G protein-coupled receptor that is widely distributed in the central nervous system and several peripheral tissues and binds the active component of cannabis, Δ9-tetrahydrocannabinol.{6749} Signaling through the CB1 receptor is implicated in attentional and working memory deficits as well as obesity.{12559,14939,15542} AVE-1625 is a highly potent, selective antagonist for the CB1 receptor with Ki values of 0.16-0.44 nM.{15542} At 1-3 mg/kg, AVE-1625 significantly improves the performance of rodents in working memory tasks.{15542} At 30 mg/kg, AVE-1625 reduces caloric intake by more than 50% of controls and significantly increases lipolysis from fat tissues and reduces hepatic glycogen levels in rodents.{15541}  

     

    Brand:
    Cayman
    SKU:10009021 - 5 mg

    Available on backorder

  • Avenaciolide is a water-insoluble fungal metabolite originally isolated from A. avenaceus.{49167} It inhibits glutamate transport in isolated rat liver mitochondria (Ki = 8 μM).  

     

    Brand:
    Cayman
    SKU:28128 - 2.5 mg

    Available on backorder

  • Avenaciolide is a water-insoluble fungal metabolite originally isolated from A. avenaceus.{49167} It inhibits glutamate transport in isolated rat liver mitochondria (Ki = 8 μM).  

     

    Brand:
    Cayman
    SKU:28128 - 500 µg

    Available on backorder

  • Avenanthramide-C methyl ester is an inhibitor of NF-κB activation that acts by blocking the phosphorylation of IKK and IκB (IC50 ~ 40 μM).{15451} Through this mechanism, avenanthramide-C methyl ester dose dependently inhibits the expression and secretion of IL-6, IL-8, and MCP-1 in human aortic endothelial cells. {15451}  

     

    Brand:
    Cayman
    SKU:10011336 - 1 mg

    Available on backorder

  • Avenanthramide-C methyl ester is an inhibitor of NF-κB activation that acts by blocking the phosphorylation of IKK and IκB (IC50 ~ 40 μM).{15451} Through this mechanism, avenanthramide-C methyl ester dose dependently inhibits the expression and secretion of IL-6, IL-8, and MCP-1 in human aortic endothelial cells. {15451}  

     

    Brand:
    Cayman
    SKU:10011336 - 10 mg

    Available on backorder

  • Avenanthramide-C methyl ester is an inhibitor of NF-κB activation that acts by blocking the phosphorylation of IKK and IκB (IC50 ~ 40 μM).{15451} Through this mechanism, avenanthramide-C methyl ester dose dependently inhibits the expression and secretion of IL-6, IL-8, and MCP-1 in human aortic endothelial cells. {15451}  

     

    Brand:
    Cayman
    SKU:10011336 - 5 mg

    Available on backorder

  • Avenanthramide-C methyl ester is an inhibitor of NF-κB activation that acts by blocking the phosphorylation of IKK and IκB (IC50 ~ 40 μM).{15451} Through this mechanism, avenanthramide-C methyl ester dose dependently inhibits the expression and secretion of IL-6, IL-8, and MCP-1 in human aortic endothelial cells. {15451}  

     

    Brand:
    Cayman
    SKU:10011336 - 500 µg

    Available on backorder

  • Averantin is an anthraquinone fungal metabolite that has been found in Aspergillus.{48478,48479} It is an intermediate in the biosynthesis of aflatoxin B1 (Item No. 11293).{48478} Averantin is active against B. subtilis bacteria and the plant pathogenic fungus F. solani in vitro (MICs = 16-32 μg/ml).{48479}  

     

    Brand:
    Cayman
    SKU:28059 - 5 mg

    Available on backorder

  • Avermectin B1a is a macrocyclic lactone disaccharide anthelmintic agent that binds to high and low affinity sites on the mammalian GABAA receptor.{35015,35017,35019} Binding to the high affinity site activates the receptor to increase chloride influx, while binding to the low affinity site blocks the channel.{35019} Avermectin B1a inhibits binding of the glycine receptor antagonist strychnine to membranes and the solubilized receptor from rat spinal cord (Kis = 1.3 and 3.6 µM, respectively).{35020} Formulations containing avermectin B1a (>80%) and avermectin B1b (~20%; Item No. 17453) are used in insecticides and veterinary anthelmintic formulas as abamectin (Item No. 19201).{35016,35018}  

     

    Brand:
    Cayman
    SKU:22000 -

    Out of stock

  • Avermectin B1a is a macrocyclic lactone disaccharide anthelmintic agent that binds to high and low affinity sites on the mammalian GABAA receptor.{35015,35017,35019} Binding to the high affinity site activates the receptor to increase chloride influx, while binding to the low affinity site blocks the channel.{35019} Avermectin B1a inhibits binding of the glycine receptor antagonist strychnine to membranes and the solubilized receptor from rat spinal cord (Kis = 1.3 and 3.6 µM, respectively).{35020} Formulations containing avermectin B1a (>80%) and avermectin B1b (~20%; Item No. 17453) are used in insecticides and veterinary anthelmintic formulas as abamectin (Item No. 19201).{35016,35018}  

     

    Brand:
    Cayman
    SKU:22000 -

    Out of stock

  • Avermectin B1a is a macrocyclic lactone disaccharide anthelmintic agent that binds to high and low affinity sites on the mammalian GABAA receptor.{35015,35017,35019} Binding to the high affinity site activates the receptor to increase chloride influx, while binding to the low affinity site blocks the channel.{35019} Avermectin B1a inhibits binding of the glycine receptor antagonist strychnine to membranes and the solubilized receptor from rat spinal cord (Kis = 1.3 and 3.6 µM, respectively).{35020} Formulations containing avermectin B1a (>80%) and avermectin B1b (~20%; Item No. 17453) are used in insecticides and veterinary anthelmintic formulas as abamectin (Item No. 19201).{35016,35018}  

     

    Brand:
    Cayman
    SKU:22000 -

    Out of stock

  • Avermectin B1a is a macrocyclic lactone disaccharide anthelmintic agent that binds to high and low affinity sites on the mammalian GABAA receptor.{35015,35017,35019} Binding to the high affinity site activates the receptor to increase chloride influx, while binding to the low affinity site blocks the channel.{35019} Avermectin B1a inhibits binding of the glycine receptor antagonist strychnine to membranes and the solubilized receptor from rat spinal cord (Kis = 1.3 and 3.6 µM, respectively).{35020} Formulations containing avermectin B1a (>80%) and avermectin B1b (~20%; Item No. 17453) are used in insecticides and veterinary anthelmintic formulas as abamectin (Item No. 19201).{35016,35018}  

     

    Brand:
    Cayman
    SKU:22000 -

    Out of stock

  • Avermectin B1a aglycone is an aglycone form of the anthelmintic and insecticide avermectin B1a (Item No. 22000).{46109} It hyperpolarizes P. crassipes muscle fibers with a minimum active concentration (MAC) value of 0.1 μM. Avermectin B1a aglycone decreases survival of C. elegans (MAC = 0.1 μM). In vivo, avermectin B1a aglycone prevents seizures induced by pentylenetetrazole (PTZ; Item No. 18682) in mice (ED50 = 43.9 mg/kg) without inducing deficits in rotarod performance.{35146}  

     

    Brand:
    Cayman
    SKU:28051 - 1 mg

    Available on backorder

  • Avermectin B1a aglycone is an aglycone form of the anthelmintic and insecticide avermectin B1a (Item No. 22000).{46109} It hyperpolarizes P. crassipes muscle fibers with a minimum active concentration (MAC) value of 0.1 μM. Avermectin B1a aglycone decreases survival of C. elegans (MAC = 0.1 μM). In vivo, avermectin B1a aglycone prevents seizures induced by pentylenetetrazole (PTZ; Item No. 18682) in mice (ED50 = 43.9 mg/kg) without inducing deficits in rotarod performance.{35146}  

     

    Brand:
    Cayman
    SKU:28051 - 5 mg

    Available on backorder

  • Avermectins are insecticides and anthelmintics first isolated from broths fermented by S. avermitilis.{28251} They potentiate glutamate- and GABA-gated chloride channel opening in nematodes.{26993,28250} Avermectin B1b is a minor component of avermectin broth.{26993} Avermectins, including avermectin B1b, are used broadly against nematodes, ticks, flies, and ants.{26993}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • Avermectins are insecticides and anthelmintics first isolated from broths fermented by S. avermitilis.{28251} They potentiate glutamate- and GABA-gated chloride channel opening in nematodes.{26993,28250} Avermectin B1b is a minor component of avermectin broth.{26993} Avermectins, including avermectin B1b, are used broadly against nematodes, ticks, flies, and ants.{26993}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • Avibactam is a β-lactamase inhibitor (IC50s = 8, 80, and 38 nM for TEM-1, P99, and KPC-2 β-lactamases, respectively).{39116,39113} It restores the antimicrobial activity of ceftazidime (Item No. 14828), ceftriaxone (Item No. 18866), imipenem (Item No. 16039), and piperacillin (Item No. 20766) against antibiotic-resistant Enterobacteriaceae in vitro (MIC90 reduction 4-1,024-fold across 190 E. coli and K. pneumoniae clinical isolates).{39114} Formulations containing avibactam have been used to treat carbapenem-resistant Enterobacteriaceae infections.{39115}  

     

    Brand:
    Cayman
    SKU:22825 -

    Out of stock

  • Avibactam is a β-lactamase inhibitor (IC50s = 8, 80, and 38 nM for TEM-1, P99, and KPC-2 β-lactamases, respectively).{39116,39113} It restores the antimicrobial activity of ceftazidime (Item No. 14828), ceftriaxone (Item No. 18866), imipenem (Item No. 16039), and piperacillin (Item No. 20766) against antibiotic-resistant Enterobacteriaceae in vitro (MIC90 reduction 4-1,024-fold across 190 E. coli and K. pneumoniae clinical isolates).{39114} Formulations containing avibactam have been used to treat carbapenem-resistant Enterobacteriaceae infections.{39115}  

     

    Brand:
    Cayman
    SKU:22825 -

    Out of stock

  • Avibactam is a β-lactamase inhibitor (IC50s = 8, 80, and 38 nM for TEM-1, P99, and KPC-2 β-lactamases, respectively).{39116,39113} It restores the antimicrobial activity of ceftazidime (Item No. 14828), ceftriaxone (Item No. 18866), imipenem (Item No. 16039), and piperacillin (Item No. 20766) against antibiotic-resistant Enterobacteriaceae in vitro (MIC90 reduction 4-1,024-fold across 190 E. coli and K. pneumoniae clinical isolates).{39114} Formulations containing avibactam have been used to treat carbapenem-resistant Enterobacteriaceae infections.{39115}  

     

    Brand:
    Cayman
    SKU:22825 -

    Out of stock

  • Avibactam is a β-lactamase inhibitor (IC50s = 8, 80, and 38 nM for TEM-1, P99, and KPC-2 β-lactamases, respectively).{39116,39113} It restores the antimicrobial activity of ceftazidime (Item No. 14828), ceftriaxone (Item No. 18866), imipenem (Item No. 16039), and piperacillin (Item No. 20766) against antibiotic-resistant Enterobacteriaceae in vitro (MIC90 reduction 4-1,024-fold across 190 E. coli and K. pneumoniae clinical isolates).{39114} Formulations containing avibactam have been used to treat carbapenem-resistant Enterobacteriaceae infections.{39115}  

     

    Brand:
    Cayman
    SKU:22825 -

    Out of stock

  • Avilamycin A is an antibiotic.{45579} It is active against veterinary isolates of C. perfringens (MICs = ≤0.06-0.5 mg/L) and B. hyodysenteriae (MICs = 12.5-100 μg/ml).{45579,45580} Dietary administration of avilamycin A (15 and 30 ppm) reduces mortality in a broiler cockerel model of C. perfringens infection.{45581} Formulations containing avilamycin A have been used in the prevention of necrotic enteritis in livestock.  

     

    Brand:
    Cayman
    SKU:29135 - 10 mg

    Available on backorder

  • Avilamycin A is an antibiotic.{45579} It is active against veterinary isolates of C. perfringens (MICs = ≤0.06-0.5 mg/L) and B. hyodysenteriae (MICs = 12.5-100 μg/ml).{45579,45580} Dietary administration of avilamycin A (15 and 30 ppm) reduces mortality in a broiler cockerel model of C. perfringens infection.{45581} Formulations containing avilamycin A have been used in the prevention of necrotic enteritis in livestock.  

     

    Brand:
    Cayman
    SKU:29135 - 25 mg

    Available on backorder

  • Avilamycin A is an antibiotic.{45579} It is active against veterinary isolates of C. perfringens (MICs = ≤0.06-0.5 mg/L) and B. hyodysenteriae (MICs = 12.5-100 μg/ml).{45579,45580} Dietary administration of avilamycin A (15 and 30 ppm) reduces mortality in a broiler cockerel model of C. perfringens infection.{45581} Formulations containing avilamycin A have been used in the prevention of necrotic enteritis in livestock.  

     

    Brand:
    Cayman
    SKU:29135 - 5 mg

    Available on backorder

  • Avilamycin A is an antibiotic.{45579} It is active against veterinary isolates of C. perfringens (MICs = ≤0.06-0.5 mg/L) and B. hyodysenteriae (MICs = 12.5-100 μg/ml).{45579,45580} Dietary administration of avilamycin A (15 and 30 ppm) reduces mortality in a broiler cockerel model of C. perfringens infection.{45581} Formulations containing avilamycin A have been used in the prevention of necrotic enteritis in livestock.  

     

    Brand:
    Cayman
    SKU:29135 - 50 mg

    Available on backorder

  • Avitinib is a pyrrolopyrimidine-based, irreversible inhibitor of the epidermal growth factor receptor (EGFR). It is selective for EGFR-active and T790M mutations, exhibiting a 298-fold increase in potency compared with wild-type EGFR.{33610} In a xenograft model, oral administration of 500 mg/kg avitinib was shown to result in complete remission of tumors with EGFR-active and T790M mutations.{33610}  

     

    Brand:
    Cayman
    SKU:21387 -

    Out of stock

  • Avitinib is a pyrrolopyrimidine-based, irreversible inhibitor of the epidermal growth factor receptor (EGFR). It is selective for EGFR-active and T790M mutations, exhibiting a 298-fold increase in potency compared with wild-type EGFR.{33610} In a xenograft model, oral administration of 500 mg/kg avitinib was shown to result in complete remission of tumors with EGFR-active and T790M mutations.{33610}  

     

    Brand:
    Cayman
    SKU:21387 -

    Out of stock

  • Avitinib is a pyrrolopyrimidine-based, irreversible inhibitor of the epidermal growth factor receptor (EGFR). It is selective for EGFR-active and T790M mutations, exhibiting a 298-fold increase in potency compared with wild-type EGFR.{33610} In a xenograft model, oral administration of 500 mg/kg avitinib was shown to result in complete remission of tumors with EGFR-active and T790M mutations.{33610}  

     

    Brand:
    Cayman
    SKU:21387 -

    Out of stock

  • Avitinib is a pyrrolopyrimidine-based, irreversible inhibitor of the epidermal growth factor receptor (EGFR). It is selective for EGFR-active and T790M mutations, exhibiting a 298-fold increase in potency compared with wild-type EGFR.{33610} In a xenograft model, oral administration of 500 mg/kg avitinib was shown to result in complete remission of tumors with EGFR-active and T790M mutations.{33610}  

     

    Brand:
    Cayman
    SKU:21387 -

    Out of stock

  • Bruton’s tyrosine kinase (BTK) is a non-receptor tyrosine kinase involved in signal transduction pathways regulating the proliferation, activation, and differentiation of B cells. AVL-292 is an orally available, selective, and irreversible inhibitor of BTK (IC50 = 0.5 nM in vitro in B cell lymphoma cell lines) that targets and covalently binds to BTK at cysteine-481, thereby preventing its activity.{30733,30731} AVL-292 has been shown to inhibit osteoclast function and to reduce osteoclast-stimulated proliferation of multiple myeloma cells in animal models of rheumatoid arthritis and multiple sclerosis, both of which are diseases where B cells play an important role.{30731,30732} In clinical trials, AVL-292 has demonstrated therapeutic significance in the treatment of both B cell-related cancers (e.g., non-Hodgkin’s lymphoma and B cell chronic lymphocytic leukemia) and autoimmune diseases (e.g., rheumatoid arthritis).{30731,30642,30732}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • Bruton’s tyrosine kinase (BTK) is a non-receptor tyrosine kinase involved in signal transduction pathways regulating the proliferation, activation, and differentiation of B cells. AVL-292 is an orally available, selective, and irreversible inhibitor of BTK (IC50 = 0.5 nM in vitro in B cell lymphoma cell lines) that targets and covalently binds to BTK at cysteine-481, thereby preventing its activity.{30733,30731} AVL-292 has been shown to inhibit osteoclast function and to reduce osteoclast-stimulated proliferation of multiple myeloma cells in animal models of rheumatoid arthritis and multiple sclerosis, both of which are diseases where B cells play an important role.{30731,30732} In clinical trials, AVL-292 has demonstrated therapeutic significance in the treatment of both B cell-related cancers (e.g., non-Hodgkin’s lymphoma and B cell chronic lymphocytic leukemia) and autoimmune diseases (e.g., rheumatoid arthritis).{30731,30642,30732}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • Bruton’s tyrosine kinase (BTK) is a non-receptor tyrosine kinase involved in signal transduction pathways regulating the proliferation, activation, and differentiation of B cells. AVL-292 is an orally available, selective, and irreversible inhibitor of BTK (IC50 = 0.5 nM in vitro in B cell lymphoma cell lines) that targets and covalently binds to BTK at cysteine-481, thereby preventing its activity.{30733,30731} AVL-292 has been shown to inhibit osteoclast function and to reduce osteoclast-stimulated proliferation of multiple myeloma cells in animal models of rheumatoid arthritis and multiple sclerosis, both of which are diseases where B cells play an important role.{30731,30732} In clinical trials, AVL-292 has demonstrated therapeutic significance in the treatment of both B cell-related cancers (e.g., non-Hodgkin’s lymphoma and B cell chronic lymphocytic leukemia) and autoimmune diseases (e.g., rheumatoid arthritis).{30731,30642,30732}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • Bruton’s tyrosine kinase (BTK) is a non-receptor tyrosine kinase involved in signal transduction pathways regulating the proliferation, activation, and differentiation of B cells. AVL-292 is an orally available, selective, and irreversible inhibitor of BTK (IC50 = 0.5 nM in vitro in B cell lymphoma cell lines) that targets and covalently binds to BTK at cysteine-481, thereby preventing its activity.{30733,30731} AVL-292 has been shown to inhibit osteoclast function and to reduce osteoclast-stimulated proliferation of multiple myeloma cells in animal models of rheumatoid arthritis and multiple sclerosis, both of which are diseases where B cells play an important role.{30731,30732} In clinical trials, AVL-292 has demonstrated therapeutic significance in the treatment of both B cell-related cancers (e.g., non-Hodgkin’s lymphoma and B cell chronic lymphocytic leukemia) and autoimmune diseases (e.g., rheumatoid arthritis).{30731,30642,30732}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • AVN-492 is an antagonist of the serotonin (5-HT) receptor subtype 5-HT6 (Ki = 0.09 nM).{52052} It selectively inhibits the 5-HT6 receptor over the 5-HT2B receptor (IC50s = 0.19 and 268 nM, respectively, in a radioligand binding assay). AVN-492 inhibits increases in cAMP levels induced by 5-HT in HEK293 cells expressing the 5-HT6 receptor (IC50 = 1.5 nM). It increases the time spent in the open arms of the elevated plus maze in rats, indicating anxiolytic activity, when administered at a dose of 0.2 mg/kg. AVN-492 (1 mg/kg) also prevents memory deficits induced by the NMDA receptor antagonist MK-801 in a passive avoidance test.  

     

    Brand:
    Cayman
    SKU:28079 - 1 mg

    Available on backorder

  • AVN-492 is an antagonist of the serotonin (5-HT) receptor subtype 5-HT6 (Ki = 0.09 nM).{52052} It selectively inhibits the 5-HT6 receptor over the 5-HT2B receptor (IC50s = 0.19 and 268 nM, respectively, in a radioligand binding assay). AVN-492 inhibits increases in cAMP levels induced by 5-HT in HEK293 cells expressing the 5-HT6 receptor (IC50 = 1.5 nM). It increases the time spent in the open arms of the elevated plus maze in rats, indicating anxiolytic activity, when administered at a dose of 0.2 mg/kg. AVN-492 (1 mg/kg) also prevents memory deficits induced by the NMDA receptor antagonist MK-801 in a passive avoidance test.  

     

    Brand:
    Cayman
    SKU:28079 - 10 mg

    Available on backorder

  • AVN-492 is an antagonist of the serotonin (5-HT) receptor subtype 5-HT6 (Ki = 0.09 nM).{52052} It selectively inhibits the 5-HT6 receptor over the 5-HT2B receptor (IC50s = 0.19 and 268 nM, respectively, in a radioligand binding assay). AVN-492 inhibits increases in cAMP levels induced by 5-HT in HEK293 cells expressing the 5-HT6 receptor (IC50 = 1.5 nM). It increases the time spent in the open arms of the elevated plus maze in rats, indicating anxiolytic activity, when administered at a dose of 0.2 mg/kg. AVN-492 (1 mg/kg) also prevents memory deficits induced by the NMDA receptor antagonist MK-801 in a passive avoidance test.  

     

    Brand:
    Cayman
    SKU:28079 - 25 mg

    Available on backorder

  • AVN-492 is an antagonist of the serotonin (5-HT) receptor subtype 5-HT6 (Ki = 0.09 nM).{52052} It selectively inhibits the 5-HT6 receptor over the 5-HT2B receptor (IC50s = 0.19 and 268 nM, respectively, in a radioligand binding assay). AVN-492 inhibits increases in cAMP levels induced by 5-HT in HEK293 cells expressing the 5-HT6 receptor (IC50 = 1.5 nM). It increases the time spent in the open arms of the elevated plus maze in rats, indicating anxiolytic activity, when administered at a dose of 0.2 mg/kg. AVN-492 (1 mg/kg) also prevents memory deficits induced by the NMDA receptor antagonist MK-801 in a passive avoidance test.  

     

    Brand:
    Cayman
    SKU:28079 - 5 mg

    Available on backorder

  • AVN944 is a selective, noncompetitive inhibitor of inosine-5′-monophosphate dehydrogenase (IMPDH; Ki = 6-10 nM for both human IMPDH isoforms), a rate-limiting enzyme involved in the de novo synthesis of purine nucleotides.{33492} Inhibition of IMPDH results in disruption of DNA and RNA synthesis, inhibition of cell proliferation, and the induction of apoptosis. AVN944 has been shown to inhibit the proliferation of multiple myeloma cells in vitro by inducing caspase-independent apoptosis.{33492} It is also reported to have antitumor properties in androgen-sensitive and androgen-independent prostate cancer cells in vitro.{33491}  

     

    Brand:
    Cayman
    SKU:21284 -

    Out of stock

  • AVN944 is a selective, noncompetitive inhibitor of inosine-5′-monophosphate dehydrogenase (IMPDH; Ki = 6-10 nM for both human IMPDH isoforms), a rate-limiting enzyme involved in the de novo synthesis of purine nucleotides.{33492} Inhibition of IMPDH results in disruption of DNA and RNA synthesis, inhibition of cell proliferation, and the induction of apoptosis. AVN944 has been shown to inhibit the proliferation of multiple myeloma cells in vitro by inducing caspase-independent apoptosis.{33492} It is also reported to have antitumor properties in androgen-sensitive and androgen-independent prostate cancer cells in vitro.{33491}  

     

    Brand:
    Cayman
    SKU:21284 -

    Out of stock

  • AVN944 is a selective, noncompetitive inhibitor of inosine-5′-monophosphate dehydrogenase (IMPDH; Ki = 6-10 nM for both human IMPDH isoforms), a rate-limiting enzyme involved in the de novo synthesis of purine nucleotides.{33492} Inhibition of IMPDH results in disruption of DNA and RNA synthesis, inhibition of cell proliferation, and the induction of apoptosis. AVN944 has been shown to inhibit the proliferation of multiple myeloma cells in vitro by inducing caspase-independent apoptosis.{33492} It is also reported to have antitumor properties in androgen-sensitive and androgen-independent prostate cancer cells in vitro.{33491}  

     

    Brand:
    Cayman
    SKU:21284 -

    Out of stock

  • AVN944 is a selective, noncompetitive inhibitor of inosine-5′-monophosphate dehydrogenase (IMPDH; Ki = 6-10 nM for both human IMPDH isoforms), a rate-limiting enzyme involved in the de novo synthesis of purine nucleotides.{33492} Inhibition of IMPDH results in disruption of DNA and RNA synthesis, inhibition of cell proliferation, and the induction of apoptosis. AVN944 has been shown to inhibit the proliferation of multiple myeloma cells in vitro by inducing caspase-independent apoptosis.{33492} It is also reported to have antitumor properties in androgen-sensitive and androgen-independent prostate cancer cells in vitro.{33491}  

     

    Brand:
    Cayman
    SKU:21284 -

    Out of stock

  • Avobenzone is a full-spectrum ultraviolet A (UVA) blocker.{41451} It inhibits UVA-induced melanin and tyrosinase activity in B16/F10 melanoma cells (IC30s = 21.94 and 24.25 μM, respectively).{41452} Avobenzone (30 μM) also inhibits UVA-induced production of reactive oxygen species (ROS) and 8-hydroxy-2′-deoxyguanosine (8-OH-dG; Item No. 89320) and depletion of glutathione (GSH; Item No. 10007461) in B16/F10 cells. It increases nuclear translocation of nuclear factor (erythroid-derived 2)-like 2 (Nrf2) and upregulates the antioxidant response element (ARE) in UVA-irradiated B16/F10 cells at a concentration of 30 μM. Formulations containing avobenzone have been used as a sun protectant in sunscreen products.  

     

    Brand:
    Cayman
    SKU:23836 - 10 g

    Available on backorder

  • Avobenzone is a full-spectrum ultraviolet A (UVA) blocker.{41451} It inhibits UVA-induced melanin and tyrosinase activity in B16/F10 melanoma cells (IC30s = 21.94 and 24.25 μM, respectively).{41452} Avobenzone (30 μM) also inhibits UVA-induced production of reactive oxygen species (ROS) and 8-hydroxy-2′-deoxyguanosine (8-OH-dG; Item No. 89320) and depletion of glutathione (GSH; Item No. 10007461) in B16/F10 cells. It increases nuclear translocation of nuclear factor (erythroid-derived 2)-like 2 (Nrf2) and upregulates the antioxidant response element (ARE) in UVA-irradiated B16/F10 cells at a concentration of 30 μM. Formulations containing avobenzone have been used as a sun protectant in sunscreen products.  

     

    Brand:
    Cayman
    SKU:23836 - 100 g

    Available on backorder

  • Avobenzone is a full-spectrum ultraviolet A (UVA) blocker.{41451} It inhibits UVA-induced melanin and tyrosinase activity in B16/F10 melanoma cells (IC30s = 21.94 and 24.25 μM, respectively).{41452} Avobenzone (30 μM) also inhibits UVA-induced production of reactive oxygen species (ROS) and 8-hydroxy-2′-deoxyguanosine (8-OH-dG; Item No. 89320) and depletion of glutathione (GSH; Item No. 10007461) in B16/F10 cells. It increases nuclear translocation of nuclear factor (erythroid-derived 2)-like 2 (Nrf2) and upregulates the antioxidant response element (ARE) in UVA-irradiated B16/F10 cells at a concentration of 30 μM. Formulations containing avobenzone have been used as a sun protectant in sunscreen products.  

     

    Brand:
    Cayman
    SKU:23836 - 25 g

    Available on backorder

  • Avobenzone is a full-spectrum ultraviolet A (UVA) blocker.{41451} It inhibits UVA-induced melanin and tyrosinase activity in B16/F10 melanoma cells (IC30s = 21.94 and 24.25 μM, respectively).{41452} Avobenzone (30 μM) also inhibits UVA-induced production of reactive oxygen species (ROS) and 8-hydroxy-2′-deoxyguanosine (8-OH-dG; Item No. 89320) and depletion of glutathione (GSH; Item No. 10007461) in B16/F10 cells. It increases nuclear translocation of nuclear factor (erythroid-derived 2)-like 2 (Nrf2) and upregulates the antioxidant response element (ARE) in UVA-irradiated B16/F10 cells at a concentration of 30 μM. Formulations containing avobenzone have been used as a sun protectant in sunscreen products.  

     

    Brand:
    Cayman
    SKU:23836 - 5 g

    Available on backorder

  • Avridine is a synthetic lipid amine that acts as an adjuvant.{48943} Subplantar injection of avridine induces paw swelling, an effect that can be blocked by the non-steroidal anti-inflammatory drug (NSAID) phenylbutazone (Item No. 70400) or the alkylating agent cyclophosphamide (Item No. 13849), in rats. Avridine induces paw joint tissue destruction, bone and pannus formation, and neutrophil, fibroblast, and osteoclast infiltration in the same model. It also increases the number of CD4+ T and MHC class II+ cells in rat paws when administered at a dose of 1.5 mg/animal.{48944} Avridine has been used to induce experimental rheumatoid arthritis in rats.{48944,48945,48946}  

     

    Brand:
    Cayman
    SKU:30198 - 1 mg

    Available on backorder

  • Avridine is a synthetic lipid amine that acts as an adjuvant.{48943} Subplantar injection of avridine induces paw swelling, an effect that can be blocked by the non-steroidal anti-inflammatory drug (NSAID) phenylbutazone (Item No. 70400) or the alkylating agent cyclophosphamide (Item No. 13849), in rats. Avridine induces paw joint tissue destruction, bone and pannus formation, and neutrophil, fibroblast, and osteoclast infiltration in the same model. It also increases the number of CD4+ T and MHC class II+ cells in rat paws when administered at a dose of 1.5 mg/animal.{48944} Avridine has been used to induce experimental rheumatoid arthritis in rats.{48944,48945,48946}  

     

    Brand:
    Cayman
    SKU:30198 - 10 mg

    Available on backorder

  • Avridine is a synthetic lipid amine that acts as an adjuvant.{48943} Subplantar injection of avridine induces paw swelling, an effect that can be blocked by the non-steroidal anti-inflammatory drug (NSAID) phenylbutazone (Item No. 70400) or the alkylating agent cyclophosphamide (Item No. 13849), in rats. Avridine induces paw joint tissue destruction, bone and pannus formation, and neutrophil, fibroblast, and osteoclast infiltration in the same model. It also increases the number of CD4+ T and MHC class II+ cells in rat paws when administered at a dose of 1.5 mg/animal.{48944} Avridine has been used to induce experimental rheumatoid arthritis in rats.{48944,48945,48946}  

     

    Brand:
    Cayman
    SKU:30198 - 25 mg

    Available on backorder

  • Avridine is a synthetic lipid amine that acts as an adjuvant.{48943} Subplantar injection of avridine induces paw swelling, an effect that can be blocked by the non-steroidal anti-inflammatory drug (NSAID) phenylbutazone (Item No. 70400) or the alkylating agent cyclophosphamide (Item No. 13849), in rats. Avridine induces paw joint tissue destruction, bone and pannus formation, and neutrophil, fibroblast, and osteoclast infiltration in the same model. It also increases the number of CD4+ T and MHC class II+ cells in rat paws when administered at a dose of 1.5 mg/animal.{48944} Avridine has been used to induce experimental rheumatoid arthritis in rats.{48944,48945,48946}  

     

    Brand:
    Cayman
    SKU:30198 - 5 mg

    Available on backorder

  • AWD 131-138 is a partial agonist of the GABAA receptor that acts at the benzodiazepine binding site, dose-dependently stimulating GABA currents with a threshold of 0.3-1.0 µM.{29595} This effect is blocked by the benzodiazepine antagonist flumazenil (Item No. 14252).{29595} AWD 131-138 displays a broad spectrum of anticonvulsant activity in diverse seizure and epilepsy models without a tendency toward tolerance or abuse.{29593,29594,29596} It has a superior pharmacokinetic profile in dogs vs. humans.{29594,29592}  

     

    Brand:
    Cayman
    SKU:-
  • AWD 131-138 is a partial agonist of the GABAA receptor that acts at the benzodiazepine binding site, dose-dependently stimulating GABA currents with a threshold of 0.3-1.0 µM.{29595} This effect is blocked by the benzodiazepine antagonist flumazenil (Item No. 14252).{29595} AWD 131-138 displays a broad spectrum of anticonvulsant activity in diverse seizure and epilepsy models without a tendency toward tolerance or abuse.{29593,29594,29596} It has a superior pharmacokinetic profile in dogs vs. humans.{29594,29592}  

     

    Brand:
    Cayman
    SKU:-
  • AWD 131-138 is a partial agonist of the GABAA receptor that acts at the benzodiazepine binding site, dose-dependently stimulating GABA currents with a threshold of 0.3-1.0 µM.{29595} This effect is blocked by the benzodiazepine antagonist flumazenil (Item No. 14252).{29595} AWD 131-138 displays a broad spectrum of anticonvulsant activity in diverse seizure and epilepsy models without a tendency toward tolerance or abuse.{29593,29594,29596} It has a superior pharmacokinetic profile in dogs vs. humans.{29594,29592}  

     

    Brand:
    Cayman
    SKU:-
  • AWD 131-138 is a partial agonist of the GABAA receptor that acts at the benzodiazepine binding site, dose-dependently stimulating GABA currents with a threshold of 0.3-1.0 µM.{29595} This effect is blocked by the benzodiazepine antagonist flumazenil (Item No. 14252).{29595} AWD 131-138 displays a broad spectrum of anticonvulsant activity in diverse seizure and epilepsy models without a tendency toward tolerance or abuse.{29593,29594,29596} It has a superior pharmacokinetic profile in dogs vs. humans.{29594,29592}  

     

    Brand:
    Cayman
    SKU:-
  • The group IVA phospholipase A2 (PLA2), known as calcium-dependent cytosolic PLA2 (cPLA2), selectively releases arachidonic acid from membrane phospholipids, playing a central role in initiating the synthesis of prostaglandins and leukotrienes.{1474} AX 048 is a potent group IVA cPLA2 inhibitor that demonstrates 50% inhibition of the enzyme at a mole fraction (XI(50)) of 0.022. Pretreatment with AX 048 (ED50 = 1.2 mg/kg) dose-dependently reduces thermal hyperalgesia evoked by carrageenan injection of rat hind paw.{18000} At concentrations as high as 30 µM, AX 048 does not inhibit COX activity or interfere with central cannabinoid receptor signaling.{18000}  

     

    Brand:
    Cayman
    SKU:-
  • The group IVA phospholipase A2 (PLA2), known as calcium-dependent cytosolic PLA2 (cPLA2), selectively releases arachidonic acid from membrane phospholipids, playing a central role in initiating the synthesis of prostaglandins and leukotrienes.{1474} AX 048 is a potent group IVA cPLA2 inhibitor that demonstrates 50% inhibition of the enzyme at a mole fraction (XI(50)) of 0.022. Pretreatment with AX 048 (ED50 = 1.2 mg/kg) dose-dependently reduces thermal hyperalgesia evoked by carrageenan injection of rat hind paw.{18000} At concentrations as high as 30 µM, AX 048 does not inhibit COX activity or interfere with central cannabinoid receptor signaling.{18000}  

     

    Brand:
    Cayman
    SKU:-
  • The group IVA phospholipase A2 (PLA2), known as calcium-dependent cytosolic PLA2 (cPLA2), selectively releases arachidonic acid from membrane phospholipids, playing a central role in initiating the synthesis of prostaglandins and leukotrienes.{1474} AX 048 is a potent group IVA cPLA2 inhibitor that demonstrates 50% inhibition of the enzyme at a mole fraction (XI(50)) of 0.022. Pretreatment with AX 048 (ED50 = 1.2 mg/kg) dose-dependently reduces thermal hyperalgesia evoked by carrageenan injection of rat hind paw.{18000} At concentrations as high as 30 µM, AX 048 does not inhibit COX activity or interfere with central cannabinoid receptor signaling.{18000}  

     

    Brand:
    Cayman
    SKU:-
  • AX-024 is an inhibitor of the CD3ε-Nck interaction.{49065} It binds to the SH3.1 N-terminal domain of Nck1, preventing its binding to the proline-rich sequence of the CD3ε subunit of T cells. AX-024 inhibits T cell receptor-triggered T cell activation (IC50 = 1 nM for human T cells) and selectively decreases proliferation of T cells over B cells. It prevents CD4+ T cell and macrophage infiltration to the cerebellum and spinal cord and improves neurological impairments in a MOG35-55 mouse model of experimental autoimmune encephalomyelitis (EAE) when administered at a dose of 10 mg/kg per day for ten days starting on the day of immunization. AX-024 (50 mg/kg) prevents the infiltration of eosinophils, macrophages, and neutrophils into the airway, as well as prevents an increase in IL-4 levels in bronchoalveolar lavage fluid (BALF), in an ovalbumin-sensitized mouse model of allergic airway disease. It does not prevent the memory T cell response to an immunodominant B8R poxvirus antigen peptide or to infection by ectromelia virus (mousepox).  

     

    Brand:
    Cayman
    SKU:27333 - 1 mg

    Available on backorder

  • AX-024 is an inhibitor of the CD3ε-Nck interaction.{49065} It binds to the SH3.1 N-terminal domain of Nck1, preventing its binding to the proline-rich sequence of the CD3ε subunit of T cells. AX-024 inhibits T cell receptor-triggered T cell activation (IC50 = 1 nM for human T cells) and selectively decreases proliferation of T cells over B cells. It prevents CD4+ T cell and macrophage infiltration to the cerebellum and spinal cord and improves neurological impairments in a MOG35-55 mouse model of experimental autoimmune encephalomyelitis (EAE) when administered at a dose of 10 mg/kg per day for ten days starting on the day of immunization. AX-024 (50 mg/kg) prevents the infiltration of eosinophils, macrophages, and neutrophils into the airway, as well as prevents an increase in IL-4 levels in bronchoalveolar lavage fluid (BALF), in an ovalbumin-sensitized mouse model of allergic airway disease. It does not prevent the memory T cell response to an immunodominant B8R poxvirus antigen peptide or to infection by ectromelia virus (mousepox).  

     

    Brand:
    Cayman
    SKU:27333 - 10 mg

    Available on backorder

  • AX-024 is an inhibitor of the CD3ε-Nck interaction.{49065} It binds to the SH3.1 N-terminal domain of Nck1, preventing its binding to the proline-rich sequence of the CD3ε subunit of T cells. AX-024 inhibits T cell receptor-triggered T cell activation (IC50 = 1 nM for human T cells) and selectively decreases proliferation of T cells over B cells. It prevents CD4+ T cell and macrophage infiltration to the cerebellum and spinal cord and improves neurological impairments in a MOG35-55 mouse model of experimental autoimmune encephalomyelitis (EAE) when administered at a dose of 10 mg/kg per day for ten days starting on the day of immunization. AX-024 (50 mg/kg) prevents the infiltration of eosinophils, macrophages, and neutrophils into the airway, as well as prevents an increase in IL-4 levels in bronchoalveolar lavage fluid (BALF), in an ovalbumin-sensitized mouse model of allergic airway disease. It does not prevent the memory T cell response to an immunodominant B8R poxvirus antigen peptide or to infection by ectromelia virus (mousepox).  

     

    Brand:
    Cayman
    SKU:27333 - 25 mg

    Available on backorder

  • AX-024 is an inhibitor of the CD3ε-Nck interaction.{49065} It binds to the SH3.1 N-terminal domain of Nck1, preventing its binding to the proline-rich sequence of the CD3ε subunit of T cells. AX-024 inhibits T cell receptor-triggered T cell activation (IC50 = 1 nM for human T cells) and selectively decreases proliferation of T cells over B cells. It prevents CD4+ T cell and macrophage infiltration to the cerebellum and spinal cord and improves neurological impairments in a MOG35-55 mouse model of experimental autoimmune encephalomyelitis (EAE) when administered at a dose of 10 mg/kg per day for ten days starting on the day of immunization. AX-024 (50 mg/kg) prevents the infiltration of eosinophils, macrophages, and neutrophils into the airway, as well as prevents an increase in IL-4 levels in bronchoalveolar lavage fluid (BALF), in an ovalbumin-sensitized mouse model of allergic airway disease. It does not prevent the memory T cell response to an immunodominant B8R poxvirus antigen peptide or to infection by ectromelia virus (mousepox).  

     

    Brand:
    Cayman
    SKU:27333 - 5 mg

    Available on backorder

  • Axitinib is a VEGFR inhibitor (IC50s = 1.2, 0.25, and 0.29 nM for VEGFR1, -2, and -3, respectively).{18372} It also inhibits c-Kit and PDGFRβ (IC50s = 1.7 and 1.6 nM, respectively). It inhibits VEGF-induced migration of and tube formation by human umbilical vein endothelial cells (HUVECs).{57053} Axitinib (1-100 mg/kg) reduces microvessel density, a marker of angiogenesis, and tumor growth in MV522 colon carcinoma, A375 melanoma, SN12C-GFP renal carcinoma, and U87 glioma mouse xenograft models in a dose-dependent manner. Formulations containing axitinib have been used in the treatment of renal cell carcinoma.  

     

    Brand:
    Cayman
    SKU:-
  • Axitinib is a VEGFR inhibitor (IC50s = 1.2, 0.25, and 0.29 nM for VEGFR1, -2, and -3, respectively).{18372} It also inhibits c-Kit and PDGFRβ (IC50s = 1.7 and 1.6 nM, respectively). It inhibits VEGF-induced migration of and tube formation by human umbilical vein endothelial cells (HUVECs).{57053} Axitinib (1-100 mg/kg) reduces microvessel density, a marker of angiogenesis, and tumor growth in MV522 colon carcinoma, A375 melanoma, SN12C-GFP renal carcinoma, and U87 glioma mouse xenograft models in a dose-dependent manner. Formulations containing axitinib have been used in the treatment of renal cell carcinoma.  

     

    Brand:
    Cayman
    SKU:-
  • Axitinib is a VEGFR inhibitor (IC50s = 1.2, 0.25, and 0.29 nM for VEGFR1, -2, and -3, respectively).{18372} It also inhibits c-Kit and PDGFRβ (IC50s = 1.7 and 1.6 nM, respectively). It inhibits VEGF-induced migration of and tube formation by human umbilical vein endothelial cells (HUVECs).{57053} Axitinib (1-100 mg/kg) reduces microvessel density, a marker of angiogenesis, and tumor growth in MV522 colon carcinoma, A375 melanoma, SN12C-GFP renal carcinoma, and U87 glioma mouse xenograft models in a dose-dependent manner. Formulations containing axitinib have been used in the treatment of renal cell carcinoma.  

     

    Brand:
    Cayman
    SKU:-
  • Axitinib sulfoxide is a major inactive metabolite of the tyrosine kinase inhibitor axitinib (Item No. 13813).{43878,43879} It is formed from axitinib primarily by the cytochrome P450 (CYP) isoform CYP3A4 with minor contributions from CYP3A5 and CYP2C19.{43878}  

     

    Brand:
    Cayman
    SKU:28042 - 1 mg

    Available on backorder

  • Axitinib sulfoxide is a major inactive metabolite of the tyrosine kinase inhibitor axitinib (Item No. 13813).{43878,43879} It is formed from axitinib primarily by the cytochrome P450 (CYP) isoform CYP3A4 with minor contributions from CYP3A5 and CYP2C19.{43878}  

     

    Brand:
    Cayman
    SKU:28042 - 5 mg

    Available on backorder

  • Axitinib-13C-d3 is intended for use as an internal standard for the quantification of axitinib (Item No. 13813) by GC- or LC-MS. Axitinib (Item No. 13813) is a VEGFR inhibitor (IC50s = 1.2, 0.25, and 0.29 nM for VEGFR1, -2, and -3, respectively).{18372} It also inhibits c-Kit and PDGFRβ (IC50s = 1.7 and 1.6 nM, respectively). It inhibits VEGF-induced migration of and tube formation by human umbilical vein endothelial cells (HUVECs).{57053} Axitinib (1-100 mg/kg) reduces microvessel density, a marker of angiogenesis, and tumor growth in MV522 colon carcinoma, A375 melanoma, SN12C-GFP renal carcinoma, and U87 glioma mouse xenograft models in a dose-dependent manner. Formulations containing axitinib have been used in the treatment of renal cell carcinoma.  

     

    Brand:
    Cayman
    SKU:26676 - 1 mg

    Available on backorder

  • Axitinib-13C-d3 is intended for use as an internal standard for the quantification of axitinib (Item No. 13813) by GC- or LC-MS. Axitinib (Item No. 13813) is a VEGFR inhibitor (IC50s = 1.2, 0.25, and 0.29 nM for VEGFR1, -2, and -3, respectively).{18372} It also inhibits c-Kit and PDGFRβ (IC50s = 1.7 and 1.6 nM, respectively). It inhibits VEGF-induced migration of and tube formation by human umbilical vein endothelial cells (HUVECs).{57053} Axitinib (1-100 mg/kg) reduces microvessel density, a marker of angiogenesis, and tumor growth in MV522 colon carcinoma, A375 melanoma, SN12C-GFP renal carcinoma, and U87 glioma mouse xenograft models in a dose-dependent manner. Formulations containing axitinib have been used in the treatment of renal cell carcinoma.  

     

    Brand:
    Cayman
    SKU:26676 - 500 µg

    Available on backorder

  • AY 9944 prevents cholesterol biosynthesis by inhibiting the 7-dehydro cholesterol Δ7-reductase (DHCR7) enzyme (IC50 = 13 nM), which interferes with the conversion of 7-dehydro cholesterol (Item No. 14612) to cholesterol.{27278,27282} Furthermore, by upregulating the expression of DHCR7, AY 9944 can block Hedgehog signaling at the level of Smoothened or by loss of Suppressor of Fused.{27279} AY 9944 inhibition of DHCR7 has been used to recapitulate phenotypes of Smith-Lemli-Opitz syndrome, a disorder brought about by mutations in the DHCR7 gene, in animal models.{27282,27280} However, AY 9944 is highly teratogenic, producing congenital defects in offspring when fed to pregnant animals.{27281}  

     

    Brand:
    Cayman
    SKU:-
  • AY 9944 prevents cholesterol biosynthesis by inhibiting the 7-dehydro cholesterol Δ7-reductase (DHCR7) enzyme (IC50 = 13 nM), which interferes with the conversion of 7-dehydro cholesterol (Item No. 14612) to cholesterol.{27278,27282} Furthermore, by upregulating the expression of DHCR7, AY 9944 can block Hedgehog signaling at the level of Smoothened or by loss of Suppressor of Fused.{27279} AY 9944 inhibition of DHCR7 has been used to recapitulate phenotypes of Smith-Lemli-Opitz syndrome, a disorder brought about by mutations in the DHCR7 gene, in animal models.{27282,27280} However, AY 9944 is highly teratogenic, producing congenital defects in offspring when fed to pregnant animals.{27281}  

     

    Brand:
    Cayman
    SKU:-
  • AY 9944 prevents cholesterol biosynthesis by inhibiting the 7-dehydro cholesterol Δ7-reductase (DHCR7) enzyme (IC50 = 13 nM), which interferes with the conversion of 7-dehydro cholesterol (Item No. 14612) to cholesterol.{27278,27282} Furthermore, by upregulating the expression of DHCR7, AY 9944 can block Hedgehog signaling at the level of Smoothened or by loss of Suppressor of Fused.{27279} AY 9944 inhibition of DHCR7 has been used to recapitulate phenotypes of Smith-Lemli-Opitz syndrome, a disorder brought about by mutations in the DHCR7 gene, in animal models.{27282,27280} However, AY 9944 is highly teratogenic, producing congenital defects in offspring when fed to pregnant animals.{27281}  

     

    Brand:
    Cayman
    SKU:-
  • AY 9944 prevents cholesterol biosynthesis by inhibiting the 7-dehydro cholesterol Δ7-reductase (DHCR7) enzyme (IC50 = 13 nM), which interferes with the conversion of 7-dehydro cholesterol (Item No. 14612) to cholesterol.{27278,27282} Furthermore, by upregulating the expression of DHCR7, AY 9944 can block Hedgehog signaling at the level of Smoothened or by loss of Suppressor of Fused.{27279} AY 9944 inhibition of DHCR7 has been used to recapitulate phenotypes of Smith-Lemli-Opitz syndrome, a disorder brought about by mutations in the DHCR7 gene, in animal models.{27282,27280} However, AY 9944 is highly teratogenic, producing congenital defects in offspring when fed to pregnant animals.{27281}  

     

    Brand:
    Cayman
    SKU:-
  • AZ 12216052 is a positive allosteric modulator of metabotropic glutamate receptor 8 (mGluR8).{53273} It potentiates glutamate-induced [35S]GTPγS binding in GHEK cells expressing human mGluR8b (EC50 = 1 μM). In a cell-based model of Parkinson’s disease, AZ 12216052 inhibits MPP+-induced decreases in the viability of undifferentiated SH-SY5Y cells when used at concentrations ranging from 0.001 to 1 μM and in retinoic acid-differentiated SH-SY5Y cells at 0.1 and 1 μM.{53274} AZ 12216052 (10 mg/kg) increases the time spent in the open areas of the elevated zero maze and reduces the acoustic startle response in mice, indicating anxiolytic-like activity in response to avoidable and unavoidable anxiogenic stimuli, respectively.{53273}  

     

    Brand:
    Cayman
    SKU:29460 - 1 mg

    Available on backorder

  • AZ 12216052 is a positive allosteric modulator of metabotropic glutamate receptor 8 (mGluR8).{53273} It potentiates glutamate-induced [35S]GTPγS binding in GHEK cells expressing human mGluR8b (EC50 = 1 μM). In a cell-based model of Parkinson’s disease, AZ 12216052 inhibits MPP+-induced decreases in the viability of undifferentiated SH-SY5Y cells when used at concentrations ranging from 0.001 to 1 μM and in retinoic acid-differentiated SH-SY5Y cells at 0.1 and 1 μM.{53274} AZ 12216052 (10 mg/kg) increases the time spent in the open areas of the elevated zero maze and reduces the acoustic startle response in mice, indicating anxiolytic-like activity in response to avoidable and unavoidable anxiogenic stimuli, respectively.{53273}  

     

    Brand:
    Cayman
    SKU:29460 - 10 mg

    Available on backorder

  • AZ 12216052 is a positive allosteric modulator of metabotropic glutamate receptor 8 (mGluR8).{53273} It potentiates glutamate-induced [35S]GTPγS binding in GHEK cells expressing human mGluR8b (EC50 = 1 μM). In a cell-based model of Parkinson’s disease, AZ 12216052 inhibits MPP+-induced decreases in the viability of undifferentiated SH-SY5Y cells when used at concentrations ranging from 0.001 to 1 μM and in retinoic acid-differentiated SH-SY5Y cells at 0.1 and 1 μM.{53274} AZ 12216052 (10 mg/kg) increases the time spent in the open areas of the elevated zero maze and reduces the acoustic startle response in mice, indicating anxiolytic-like activity in response to avoidable and unavoidable anxiogenic stimuli, respectively.{53273}  

     

    Brand:
    Cayman
    SKU:29460 - 25 mg

    Available on backorder

  • AZ 12216052 is a positive allosteric modulator of metabotropic glutamate receptor 8 (mGluR8).{53273} It potentiates glutamate-induced [35S]GTPγS binding in GHEK cells expressing human mGluR8b (EC50 = 1 μM). In a cell-based model of Parkinson’s disease, AZ 12216052 inhibits MPP+-induced decreases in the viability of undifferentiated SH-SY5Y cells when used at concentrations ranging from 0.001 to 1 μM and in retinoic acid-differentiated SH-SY5Y cells at 0.1 and 1 μM.{53274} AZ 12216052 (10 mg/kg) increases the time spent in the open areas of the elevated zero maze and reduces the acoustic startle response in mice, indicating anxiolytic-like activity in response to avoidable and unavoidable anxiogenic stimuli, respectively.{53273}  

     

    Brand:
    Cayman
    SKU:29460 - 5 mg

    Available on backorder

  • Ataxia telangiectasia and Rad3-related protein (ATR) is a serine/threonine kinase that activates DNA processes related to the DNA damage response. AZ 20 is a potent inhibitor of ATR (IC50 = 5 nM).{28669} It displays 7.6-fold selectivity over mTOR and minimal activity against a panel of 442 other kinases, including ataxia telangiectasia mutated. AZ 20 inhibits the growth of LoVo colorectal adenocarcinoma cells in vitro. It is orally bioavailable and significantly reduces the growth of LoVo xenografts in mice.{28669}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • Ataxia telangiectasia and Rad3-related protein (ATR) is a serine/threonine kinase that activates DNA processes related to the DNA damage response. AZ 20 is a potent inhibitor of ATR (IC50 = 5 nM).{28669} It displays 7.6-fold selectivity over mTOR and minimal activity against a panel of 442 other kinases, including ataxia telangiectasia mutated. AZ 20 inhibits the growth of LoVo colorectal adenocarcinoma cells in vitro. It is orally bioavailable and significantly reduces the growth of LoVo xenografts in mice.{28669}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • Ataxia telangiectasia and Rad3-related protein (ATR) is a serine/threonine kinase that activates DNA processes related to the DNA damage response. AZ 20 is a potent inhibitor of ATR (IC50 = 5 nM).{28669} It displays 7.6-fold selectivity over mTOR and minimal activity against a panel of 442 other kinases, including ataxia telangiectasia mutated. AZ 20 inhibits the growth of LoVo colorectal adenocarcinoma cells in vitro. It is orally bioavailable and significantly reduces the growth of LoVo xenografts in mice.{28669}  

     

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    Cayman
    SKU:-

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  • Ataxia telangiectasia and Rad3-related protein (ATR) is a serine/threonine kinase that activates DNA processes related to the DNA damage response. AZ 20 is a potent inhibitor of ATR (IC50 = 5 nM).{28669} It displays 7.6-fold selectivity over mTOR and minimal activity against a panel of 442 other kinases, including ataxia telangiectasia mutated. AZ 20 inhibits the growth of LoVo colorectal adenocarcinoma cells in vitro. It is orally bioavailable and significantly reduces the growth of LoVo xenografts in mice.{28669}  

     

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    Cayman
    SKU:-

    Available on backorder

  • AZ 3146 is an inhibitor of the monopolar spindle 1 (Mps1) checkpoint kinase (IC50 = 35 nM).{33103} It displays selectivity over 46 other kinases including Cdk1 and Aurora kinase B.{33103} It has been shown to inhibit the recruitment of Mad1, Mad2, and centromere protein E (CENP-E) to kinetochores.{33103} AZ 3146 can be used with GSK923295 (Item No. 18389), an inhibitor of CENP-E, to generate aneuploidy in cells.{31964}  

     

    Brand:
    Cayman
    SKU:19991 -

    Available on backorder

  • AZ 3146 is an inhibitor of the monopolar spindle 1 (Mps1) checkpoint kinase (IC50 = 35 nM).{33103} It displays selectivity over 46 other kinases including Cdk1 and Aurora kinase B.{33103} It has been shown to inhibit the recruitment of Mad1, Mad2, and centromere protein E (CENP-E) to kinetochores.{33103} AZ 3146 can be used with GSK923295 (Item No. 18389), an inhibitor of CENP-E, to generate aneuploidy in cells.{31964}  

     

    Brand:
    Cayman
    SKU:19991 -

    Available on backorder

  • AZ 3146 is an inhibitor of the monopolar spindle 1 (Mps1) checkpoint kinase (IC50 = 35 nM).{33103} It displays selectivity over 46 other kinases including Cdk1 and Aurora kinase B.{33103} It has been shown to inhibit the recruitment of Mad1, Mad2, and centromere protein E (CENP-E) to kinetochores.{33103} AZ 3146 can be used with GSK923295 (Item No. 18389), an inhibitor of CENP-E, to generate aneuploidy in cells.{31964}  

     

    Brand:
    Cayman
    SKU:19991 -

    Available on backorder

  • AZ 3146 is an inhibitor of the monopolar spindle 1 (Mps1) checkpoint kinase (IC50 = 35 nM).{33103} It displays selectivity over 46 other kinases including Cdk1 and Aurora kinase B.{33103} It has been shown to inhibit the recruitment of Mad1, Mad2, and centromere protein E (CENP-E) to kinetochores.{33103} AZ 3146 can be used with GSK923295 (Item No. 18389), an inhibitor of CENP-E, to generate aneuploidy in cells.{31964}  

     

    Brand:
    Cayman
    SKU:19991 -

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  • AZ 33 is an inhibitor of lactate dehydrogenase A (LDHA; Kd = 0.093 μM; IC50 = 0.5 μM).{36785} It is selective for LDHA over LDHB in an NADH competition assay using recombinant enzymes (IC50s = 0.54 and 3.6 μM, respectively).{36786} AZ 33 is cell-impermeable and lacks cytotoxicity against HeLa cervical cancer cells (IC50 = >500 μM).  

     

    Brand:
    Cayman
    SKU:25444 - 1 mg

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  • AZ 33 is an inhibitor of lactate dehydrogenase A (LDHA; Kd = 0.093 μM; IC50 = 0.5 μM).{36785} It is selective for LDHA over LDHB in an NADH competition assay using recombinant enzymes (IC50s = 0.54 and 3.6 μM, respectively).{36786} AZ 33 is cell-impermeable and lacks cytotoxicity against HeLa cervical cancer cells (IC50 = >500 μM).  

     

    Brand:
    Cayman
    SKU:25444 - 10 mg

    Available on backorder

  • AZ 33 is an inhibitor of lactate dehydrogenase A (LDHA; Kd = 0.093 μM; IC50 = 0.5 μM).{36785} It is selective for LDHA over LDHB in an NADH competition assay using recombinant enzymes (IC50s = 0.54 and 3.6 μM, respectively).{36786} AZ 33 is cell-impermeable and lacks cytotoxicity against HeLa cervical cancer cells (IC50 = >500 μM).  

     

    Brand:
    Cayman
    SKU:25444 - 25 mg

    Available on backorder

  • AZ 33 is an inhibitor of lactate dehydrogenase A (LDHA; Kd = 0.093 μM; IC50 = 0.5 μM).{36785} It is selective for LDHA over LDHB in an NADH competition assay using recombinant enzymes (IC50s = 0.54 and 3.6 μM, respectively).{36786} AZ 33 is cell-impermeable and lacks cytotoxicity against HeLa cervical cancer cells (IC50 = >500 μM).  

     

    Brand:
    Cayman
    SKU:25444 - 5 mg

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  • AZ 5104 is an active, demethylated metabolite of AZD 9291 (Item No. 16237), an irreversible inhibitor of EGFR-sensitizing and T790M resistance mutations (IC50s = 15-17 nM) that spares the wild-type form of the receptor (IC50 = 480 nM).{27820,32544,32545} AZ 5104 displays a similar overall activity profile as the parent compound.{32544,32545}  

     

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    Cayman
    SKU:-

    Available on backorder

  • AZ 5104 is an active, demethylated metabolite of AZD 9291 (Item No. 16237), an irreversible inhibitor of EGFR-sensitizing and T790M resistance mutations (IC50s = 15-17 nM) that spares the wild-type form of the receptor (IC50 = 480 nM).{27820,32544,32545} AZ 5104 displays a similar overall activity profile as the parent compound.{32544,32545}  

     

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    Cayman
    SKU:-

    Available on backorder

  • AZ 5104 is an active, demethylated metabolite of AZD 9291 (Item No. 16237), an irreversible inhibitor of EGFR-sensitizing and T790M resistance mutations (IC50s = 15-17 nM) that spares the wild-type form of the receptor (IC50 = 480 nM).{27820,32544,32545} AZ 5104 displays a similar overall activity profile as the parent compound.{32544,32545}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • AZ 5104 is an active, demethylated metabolite of AZD 9291 (Item No. 16237), an irreversible inhibitor of EGFR-sensitizing and T790M resistance mutations (IC50s = 15-17 nM) that spares the wild-type form of the receptor (IC50 = 480 nM).{27820,32544,32545} AZ 5104 displays a similar overall activity profile as the parent compound.{32544,32545}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • AZ 6102 is an inhibitor of tankyrases (TNKS) 1 and 2 with IC50 values of 3 and 1 nM, respectively.{32525} It demonstrates 100-fold selectivity for TNKS1/2 over PARP1, PARP2, and PARP6 (IC50s = 2, 0.5, and >3 µM, respectively).{32525} By inhibiting TNKS1/2, AZ6120 has been shown to inhibit Wnt signaling in DLD-1 cells with an IC50 value of 5 nM.{32525}  

     

    Brand:
    Cayman
    SKU:19898 -

    Available on backorder

  • AZ 6102 is an inhibitor of tankyrases (TNKS) 1 and 2 with IC50 values of 3 and 1 nM, respectively.{32525} It demonstrates 100-fold selectivity for TNKS1/2 over PARP1, PARP2, and PARP6 (IC50s = 2, 0.5, and >3 µM, respectively).{32525} By inhibiting TNKS1/2, AZ6120 has been shown to inhibit Wnt signaling in DLD-1 cells with an IC50 value of 5 nM.{32525}  

     

    Brand:
    Cayman
    SKU:19898 -

    Available on backorder

  • AZ 6102 is an inhibitor of tankyrases (TNKS) 1 and 2 with IC50 values of 3 and 1 nM, respectively.{32525} It demonstrates 100-fold selectivity for TNKS1/2 over PARP1, PARP2, and PARP6 (IC50s = 2, 0.5, and >3 µM, respectively).{32525} By inhibiting TNKS1/2, AZ6120 has been shown to inhibit Wnt signaling in DLD-1 cells with an IC50 value of 5 nM.{32525}  

     

    Brand:
    Cayman
    SKU:19898 -

    Available on backorder

  • AZ 6102 is an inhibitor of tankyrases (TNKS) 1 and 2 with IC50 values of 3 and 1 nM, respectively.{32525} It demonstrates 100-fold selectivity for TNKS1/2 over PARP1, PARP2, and PARP6 (IC50s = 2, 0.5, and >3 µM, respectively).{32525} By inhibiting TNKS1/2, AZ6120 has been shown to inhibit Wnt signaling in DLD-1 cells with an IC50 value of 5 nM.{32525}  

     

    Brand:
    Cayman
    SKU:19898 -

    Available on backorder

  • The Raf kinases activate cellular pathways that lead to cell proliferation and can contribute to certain types of cancer.{19941,24815} Mutations in the kinase B-Raf are involved in a wide range of cancers.{18549,22622} In particular, the mutation B-RafV600E occurs in melanomas and other types of cancer but is poorly targeted by many inhibitors of wild type B-Raf.{24813,24814} AZ 628 is a quinazilinone that inhibits several Raf kinases, including B-Raf, B-RafV600E, and c-Raf-1 (IC50s = 105, 34, and 29 nM in in vitro kinase assays).{27947,27948} It also prevents activation of several tyrosine kinases, including VEGFR2, DDR2, Lyn, Flt1, and FMS.{27947} In colon and melanoma cell lines carrying B-RafV600E mutations, AZ 628 is reported to inhibit anchorage-dependent and -independent growth, induce cell cycle arrest, and cause apoptosis.{27947}  

     

    Brand:
    Cayman
    SKU:-
  • The Raf kinases activate cellular pathways that lead to cell proliferation and can contribute to certain types of cancer.{19941,24815} Mutations in the kinase B-Raf are involved in a wide range of cancers.{18549,22622} In particular, the mutation B-RafV600E occurs in melanomas and other types of cancer but is poorly targeted by many inhibitors of wild type B-Raf.{24813,24814} AZ 628 is a quinazilinone that inhibits several Raf kinases, including B-Raf, B-RafV600E, and c-Raf-1 (IC50s = 105, 34, and 29 nM in in vitro kinase assays).{27947,27948} It also prevents activation of several tyrosine kinases, including VEGFR2, DDR2, Lyn, Flt1, and FMS.{27947} In colon and melanoma cell lines carrying B-RafV600E mutations, AZ 628 is reported to inhibit anchorage-dependent and -independent growth, induce cell cycle arrest, and cause apoptosis.{27947}  

     

    Brand:
    Cayman
    SKU:-
  • The Raf kinases activate cellular pathways that lead to cell proliferation and can contribute to certain types of cancer.{19941,24815} Mutations in the kinase B-Raf are involved in a wide range of cancers.{18549,22622} In particular, the mutation B-RafV600E occurs in melanomas and other types of cancer but is poorly targeted by many inhibitors of wild type B-Raf.{24813,24814} AZ 628 is a quinazilinone that inhibits several Raf kinases, including B-Raf, B-RafV600E, and c-Raf-1 (IC50s = 105, 34, and 29 nM in in vitro kinase assays).{27947,27948} It also prevents activation of several tyrosine kinases, including VEGFR2, DDR2, Lyn, Flt1, and FMS.{27947} In colon and melanoma cell lines carrying B-RafV600E mutations, AZ 628 is reported to inhibit anchorage-dependent and -independent growth, induce cell cycle arrest, and cause apoptosis.{27947}  

     

    Brand:
    Cayman
    SKU:-
  • The Raf kinases activate cellular pathways that lead to cell proliferation and can contribute to certain types of cancer.{19941,24815} Mutations in the kinase B-Raf are involved in a wide range of cancers.{18549,22622} In particular, the mutation B-RafV600E occurs in melanomas and other types of cancer but is poorly targeted by many inhibitors of wild type B-Raf.{24813,24814} AZ 628 is a quinazilinone that inhibits several Raf kinases, including B-Raf, B-RafV600E, and c-Raf-1 (IC50s = 105, 34, and 29 nM in in vitro kinase assays).{27947,27948} It also prevents activation of several tyrosine kinases, including VEGFR2, DDR2, Lyn, Flt1, and FMS.{27947} In colon and melanoma cell lines carrying B-RafV600E mutations, AZ 628 is reported to inhibit anchorage-dependent and -independent growth, induce cell cycle arrest, and cause apoptosis.{27947}  

     

    Brand:
    Cayman
    SKU:-