Chemicals
Showing 10651–10800 of 41137 results
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MEK kinases are central components of diverse intracellular signaling pathways. MEK1 and MEK2 specifically act downstream of growth factor receptors and the proto-oncogenes Ras and Raf to activate ERK1 and ERK2, often leading to an increase in cell proliferation.{24267} AZD 6244 is a potent, highly selective inhibitor of MEK1 and MEK2 (IC50 = 14 and 530 nM, respectively).{24156,24266,24267} It weakly inhibits the EGF receptor (IC50 = 7.0 µM) and has no effect on a large panel of other kinases.{24156} AZD 6244 suppresses the growth of tumors displaying high levels of phosphorylated MEK1/2 or ERK1/2.{24266,24267} In addition to suppressing growth, it induces apoptosis and differentiation within tumors.{24265} AZD 6244 has potential, alone or in combination therapy, for promoting tumor regression in various forms of cancer, including those involving mutations of the proto-oncogenes Ras and Raf.{24269,24268}
Brand:CaymanSKU:11599 - 25 mgAvailable on backorder
MEK kinases are central components of diverse intracellular signaling pathways. MEK1 and MEK2 specifically act downstream of growth factor receptors and the proto-oncogenes Ras and Raf to activate ERK1 and ERK2, often leading to an increase in cell proliferation.{24267} AZD 6244 is a potent, highly selective inhibitor of MEK1 and MEK2 (IC50 = 14 and 530 nM, respectively).{24156,24266,24267} It weakly inhibits the EGF receptor (IC50 = 7.0 µM) and has no effect on a large panel of other kinases.{24156} AZD 6244 suppresses the growth of tumors displaying high levels of phosphorylated MEK1/2 or ERK1/2.{24266,24267} In addition to suppressing growth, it induces apoptosis and differentiation within tumors.{24265} AZD 6244 has potential, alone or in combination therapy, for promoting tumor regression in various forms of cancer, including those involving mutations of the proto-oncogenes Ras and Raf.{24269,24268}
Brand:CaymanSKU:11599 - 50 mgAvailable on backorder
AZD 6738 is an orally bioavailable inhibitor of the serine/threonine protein kinase ataxia telangiectasia mutated (ATM) and Rad3-related (ATR; IC50 = 1 nM).{32892} It can inhibit ATR substrate Chk1 Ser345 phosphorylation in cells with an IC50 value of 74 nM.{32892} AZD 6738 has been shown to inhibit the proliferation of various solid and hematological cell lines with IC50 values of less than 1 µM and to reduce tumor growth in several ATM-deficient xenograft models.{32892} When used in combination with either DNA damaging chemotherapy agents or ionizing radiation, AZD 6738 demonstrated synergistic cell killing activity across multiple cell lines in vitro and in xenograft studies.{32892}
Brand:CaymanSKU:21035 -Out of stock
AZD 6738 is an orally bioavailable inhibitor of the serine/threonine protein kinase ataxia telangiectasia mutated (ATM) and Rad3-related (ATR; IC50 = 1 nM).{32892} It can inhibit ATR substrate Chk1 Ser345 phosphorylation in cells with an IC50 value of 74 nM.{32892} AZD 6738 has been shown to inhibit the proliferation of various solid and hematological cell lines with IC50 values of less than 1 µM and to reduce tumor growth in several ATM-deficient xenograft models.{32892} When used in combination with either DNA damaging chemotherapy agents or ionizing radiation, AZD 6738 demonstrated synergistic cell killing activity across multiple cell lines in vitro and in xenograft studies.{32892}
Brand:CaymanSKU:21035 -Out of stock
AZD 6738 is an orally bioavailable inhibitor of the serine/threonine protein kinase ataxia telangiectasia mutated (ATM) and Rad3-related (ATR; IC50 = 1 nM).{32892} It can inhibit ATR substrate Chk1 Ser345 phosphorylation in cells with an IC50 value of 74 nM.{32892} AZD 6738 has been shown to inhibit the proliferation of various solid and hematological cell lines with IC50 values of less than 1 µM and to reduce tumor growth in several ATM-deficient xenograft models.{32892} When used in combination with either DNA damaging chemotherapy agents or ionizing radiation, AZD 6738 demonstrated synergistic cell killing activity across multiple cell lines in vitro and in xenograft studies.{32892}
Brand:CaymanSKU:21035 -Out of stock
AZD 6738 is an orally bioavailable inhibitor of the serine/threonine protein kinase ataxia telangiectasia mutated (ATM) and Rad3-related (ATR; IC50 = 1 nM).{32892} It can inhibit ATR substrate Chk1 Ser345 phosphorylation in cells with an IC50 value of 74 nM.{32892} AZD 6738 has been shown to inhibit the proliferation of various solid and hematological cell lines with IC50 values of less than 1 µM and to reduce tumor growth in several ATM-deficient xenograft models.{32892} When used in combination with either DNA damaging chemotherapy agents or ionizing radiation, AZD 6738 demonstrated synergistic cell killing activity across multiple cell lines in vitro and in xenograft studies.{32892}
Brand:CaymanSKU:21035 -Out of stock
AZD 7545 is an inhibitor of pyruvate dehydrogenase (PDH) kinases (PDKs), resulting in an increase in PDH activity with an EC50 value of 5.2 nM for PDK2.{31364,31365} It less potently inhibits PDK1 and PDK3 (IC50s = 87 and 600 nM, respectively).{31363} AZD 7545 stimulates pyruvate oxidation in rat hepatocytes (EC50 = 105 nM) and significantly elevates muscle PDH activity in obese Zucker rats.{31364} It elevates postprandial glucose levels and improves the 24 hour glucose profile in obese, insulin-resistant rats, compared with lean counterparts.{31364}
Brand:CaymanSKU:-Available on backorder
AZD 7545 is an inhibitor of pyruvate dehydrogenase (PDH) kinases (PDKs), resulting in an increase in PDH activity with an EC50 value of 5.2 nM for PDK2.{31364,31365} It less potently inhibits PDK1 and PDK3 (IC50s = 87 and 600 nM, respectively).{31363} AZD 7545 stimulates pyruvate oxidation in rat hepatocytes (EC50 = 105 nM) and significantly elevates muscle PDH activity in obese Zucker rats.{31364} It elevates postprandial glucose levels and improves the 24 hour glucose profile in obese, insulin-resistant rats, compared with lean counterparts.{31364}
Brand:CaymanSKU:-Available on backorder
AZD 7545 is an inhibitor of pyruvate dehydrogenase (PDH) kinases (PDKs), resulting in an increase in PDH activity with an EC50 value of 5.2 nM for PDK2.{31364,31365} It less potently inhibits PDK1 and PDK3 (IC50s = 87 and 600 nM, respectively).{31363} AZD 7545 stimulates pyruvate oxidation in rat hepatocytes (EC50 = 105 nM) and significantly elevates muscle PDH activity in obese Zucker rats.{31364} It elevates postprandial glucose levels and improves the 24 hour glucose profile in obese, insulin-resistant rats, compared with lean counterparts.{31364}
Brand:CaymanSKU:-Available on backorder
AZD 7545 is an inhibitor of pyruvate dehydrogenase (PDH) kinases (PDKs), resulting in an increase in PDH activity with an EC50 value of 5.2 nM for PDK2.{31364,31365} It less potently inhibits PDK1 and PDK3 (IC50s = 87 and 600 nM, respectively).{31363} AZD 7545 stimulates pyruvate oxidation in rat hepatocytes (EC50 = 105 nM) and significantly elevates muscle PDH activity in obese Zucker rats.{31364} It elevates postprandial glucose levels and improves the 24 hour glucose profile in obese, insulin-resistant rats, compared with lean counterparts.{31364}
Brand:CaymanSKU:-Available on backorder
AZD 7648 is an inhibitor of DNA-dependent protein kinase (DNA-PK; IC50 = 0.63 nM in an enzyme assay).{48616} It is selective for DNA-PK over TTK (IC50 = 5.012 μM), as well as JAK1, JAK2, JAK3, Aurora A, and Aurora B (IC50s = >10 μM for all). AZD 7648 reduces tumor growth in a FaDu ATM KO pharynx cancer mouse xenograft model when administered at doses of 37.5 or 75 mg/kg twice per day and induces tumor regression at these doses when administered in combination with the PARP inhibitor olaparib (Item No. 10621).
Brand:CaymanSKU:28598 - 1 mgAvailable on backorder
AZD 7648 is an inhibitor of DNA-dependent protein kinase (DNA-PK; IC50 = 0.63 nM in an enzyme assay).{48616} It is selective for DNA-PK over TTK (IC50 = 5.012 μM), as well as JAK1, JAK2, JAK3, Aurora A, and Aurora B (IC50s = >10 μM for all). AZD 7648 reduces tumor growth in a FaDu ATM KO pharynx cancer mouse xenograft model when administered at doses of 37.5 or 75 mg/kg twice per day and induces tumor regression at these doses when administered in combination with the PARP inhibitor olaparib (Item No. 10621).
Brand:CaymanSKU:28598 - 10 mgAvailable on backorder
AZD 7648 is an inhibitor of DNA-dependent protein kinase (DNA-PK; IC50 = 0.63 nM in an enzyme assay).{48616} It is selective for DNA-PK over TTK (IC50 = 5.012 μM), as well as JAK1, JAK2, JAK3, Aurora A, and Aurora B (IC50s = >10 μM for all). AZD 7648 reduces tumor growth in a FaDu ATM KO pharynx cancer mouse xenograft model when administered at doses of 37.5 or 75 mg/kg twice per day and induces tumor regression at these doses when administered in combination with the PARP inhibitor olaparib (Item No. 10621).
Brand:CaymanSKU:28598 - 25 mgAvailable on backorder
AZD 7648 is an inhibitor of DNA-dependent protein kinase (DNA-PK; IC50 = 0.63 nM in an enzyme assay).{48616} It is selective for DNA-PK over TTK (IC50 = 5.012 μM), as well as JAK1, JAK2, JAK3, Aurora A, and Aurora B (IC50s = >10 μM for all). AZD 7648 reduces tumor growth in a FaDu ATM KO pharynx cancer mouse xenograft model when administered at doses of 37.5 or 75 mg/kg twice per day and induces tumor regression at these doses when administered in combination with the PARP inhibitor olaparib (Item No. 10621).
Brand:CaymanSKU:28598 - 5 mgAvailable on backorder
Actively proliferating cells experience blocks at certain checkpoints in the cell cycle when DNA damage is detected. These checkpoints allow for DNA damage repair before further cell cycle progression. Targeting signaling pathways to selectively inhibit repair at these checkpoints in tumor cells is of considerable interest to cancer therapeutics. AZD 7762 selectively inhibits the activity of checkpoint kinases (Chk) 1 and Chk2 (IC50s = 5 nM) by competitively and reversibly binding their respective ATP-binding sites (Ki = 3.6 nM for Chk1).{20799} AZD 7762 abrogates DNA damage-induced S and G2 checkpoints with an EC50 value of 10 nM and potentiates the efficacy of DNA-damage repair prohibitive agents, gemcitabine and topotecan, both in vitro and in various tumor xenografts by modulating downstream checkpoint pathway proteins.{20799,20800,20801}
Brand:CaymanSKU:11491 - 1 mgAvailable on backorder
Actively proliferating cells experience blocks at certain checkpoints in the cell cycle when DNA damage is detected. These checkpoints allow for DNA damage repair before further cell cycle progression. Targeting signaling pathways to selectively inhibit repair at these checkpoints in tumor cells is of considerable interest to cancer therapeutics. AZD 7762 selectively inhibits the activity of checkpoint kinases (Chk) 1 and Chk2 (IC50s = 5 nM) by competitively and reversibly binding their respective ATP-binding sites (Ki = 3.6 nM for Chk1).{20799} AZD 7762 abrogates DNA damage-induced S and G2 checkpoints with an EC50 value of 10 nM and potentiates the efficacy of DNA-damage repair prohibitive agents, gemcitabine and topotecan, both in vitro and in various tumor xenografts by modulating downstream checkpoint pathway proteins.{20799,20800,20801}
Brand:CaymanSKU:11491 - 10 mgAvailable on backorder
Actively proliferating cells experience blocks at certain checkpoints in the cell cycle when DNA damage is detected. These checkpoints allow for DNA damage repair before further cell cycle progression. Targeting signaling pathways to selectively inhibit repair at these checkpoints in tumor cells is of considerable interest to cancer therapeutics. AZD 7762 selectively inhibits the activity of checkpoint kinases (Chk) 1 and Chk2 (IC50s = 5 nM) by competitively and reversibly binding their respective ATP-binding sites (Ki = 3.6 nM for Chk1).{20799} AZD 7762 abrogates DNA damage-induced S and G2 checkpoints with an EC50 value of 10 nM and potentiates the efficacy of DNA-damage repair prohibitive agents, gemcitabine and topotecan, both in vitro and in various tumor xenografts by modulating downstream checkpoint pathway proteins.{20799,20800,20801}
Brand:CaymanSKU:11491 - 25 mgAvailable on backorder
Actively proliferating cells experience blocks at certain checkpoints in the cell cycle when DNA damage is detected. These checkpoints allow for DNA damage repair before further cell cycle progression. Targeting signaling pathways to selectively inhibit repair at these checkpoints in tumor cells is of considerable interest to cancer therapeutics. AZD 7762 selectively inhibits the activity of checkpoint kinases (Chk) 1 and Chk2 (IC50s = 5 nM) by competitively and reversibly binding their respective ATP-binding sites (Ki = 3.6 nM for Chk1).{20799} AZD 7762 abrogates DNA damage-induced S and G2 checkpoints with an EC50 value of 10 nM and potentiates the efficacy of DNA-damage repair prohibitive agents, gemcitabine and topotecan, both in vitro and in various tumor xenografts by modulating downstream checkpoint pathway proteins.{20799,20800,20801}
Brand:CaymanSKU:11491 - 5 mgAvailable on backorder
AZD 8055 is a potent, selective ATP-competitive inhibitor of mTOR, exhibiting an IC50 value of 0.8 nM.{28008} It is ~1,000-fold selective for mTOR over all PI3K isoforms and exhibits no activity against a panel of 260 kinases at concentrations up to 10 µM. AZD 8055 inhibits proliferation of A549 and H838 cells with IC50 values of 53 and 20 nM, respectively. It inhibits growth of a variety of human tumor xenografts by at least 65% in mice at daily oral doses of 20 mg/kg.{28008}
Brand:CaymanSKU:-Out of stock
AZD 8055 is a potent, selective ATP-competitive inhibitor of mTOR, exhibiting an IC50 value of 0.8 nM.{28008} It is ~1,000-fold selective for mTOR over all PI3K isoforms and exhibits no activity against a panel of 260 kinases at concentrations up to 10 µM. AZD 8055 inhibits proliferation of A549 and H838 cells with IC50 values of 53 and 20 nM, respectively. It inhibits growth of a variety of human tumor xenografts by at least 65% in mice at daily oral doses of 20 mg/kg.{28008}
Brand:CaymanSKU:-Out of stock
AZD 8055 is a potent, selective ATP-competitive inhibitor of mTOR, exhibiting an IC50 value of 0.8 nM.{28008} It is ~1,000-fold selective for mTOR over all PI3K isoforms and exhibits no activity against a panel of 260 kinases at concentrations up to 10 µM. AZD 8055 inhibits proliferation of A549 and H838 cells with IC50 values of 53 and 20 nM, respectively. It inhibits growth of a variety of human tumor xenografts by at least 65% in mice at daily oral doses of 20 mg/kg.{28008}
Brand:CaymanSKU:-Out of stock
AZD 8055 is a potent, selective ATP-competitive inhibitor of mTOR, exhibiting an IC50 value of 0.8 nM.{28008} It is ~1,000-fold selective for mTOR over all PI3K isoforms and exhibits no activity against a panel of 260 kinases at concentrations up to 10 µM. AZD 8055 inhibits proliferation of A549 and H838 cells with IC50 values of 53 and 20 nM, respectively. It inhibits growth of a variety of human tumor xenografts by at least 65% in mice at daily oral doses of 20 mg/kg.{28008}
Brand:CaymanSKU:-Out of stock
AZD 8186 is a selective PI3Kβ/δ inhibitor that exhibits IC50 values of 3, 17, and 752 nM for PI3Kβ, δ, and α, respectively, in cells sensitive to isoform-specific PI3K inhibition.{33193,33194} It shows no significant binding against a panel of 442 other kinases when tested at a concentration of 10 µM and exhibits high oral efficacy in mouse cancer models.{33193} AZD 8186 inhibits growth of a range of cell lines, with preferential activity in cells with PTEN mutation or deficiency, and inhibits growth of prostate and triple negative breast cancer tumors in vivo, both as a single agent and in combination with docetaxel (Item No. 11637).{33194}
Brand:CaymanSKU:-Available on backorder
AZD 8186 is a selective PI3Kβ/δ inhibitor that exhibits IC50 values of 3, 17, and 752 nM for PI3Kβ, δ, and α, respectively, in cells sensitive to isoform-specific PI3K inhibition.{33193,33194} It shows no significant binding against a panel of 442 other kinases when tested at a concentration of 10 µM and exhibits high oral efficacy in mouse cancer models.{33193} AZD 8186 inhibits growth of a range of cell lines, with preferential activity in cells with PTEN mutation or deficiency, and inhibits growth of prostate and triple negative breast cancer tumors in vivo, both as a single agent and in combination with docetaxel (Item No. 11637).{33194}
Brand:CaymanSKU:-Available on backorder
AZD 8186 is a selective PI3Kβ/δ inhibitor that exhibits IC50 values of 3, 17, and 752 nM for PI3Kβ, δ, and α, respectively, in cells sensitive to isoform-specific PI3K inhibition.{33193,33194} It shows no significant binding against a panel of 442 other kinases when tested at a concentration of 10 µM and exhibits high oral efficacy in mouse cancer models.{33193} AZD 8186 inhibits growth of a range of cell lines, with preferential activity in cells with PTEN mutation or deficiency, and inhibits growth of prostate and triple negative breast cancer tumors in vivo, both as a single agent and in combination with docetaxel (Item No. 11637).{33194}
Brand:CaymanSKU:-Available on backorder
AZD 8186 is a selective PI3Kβ/δ inhibitor that exhibits IC50 values of 3, 17, and 752 nM for PI3Kβ, δ, and α, respectively, in cells sensitive to isoform-specific PI3K inhibition.{33193,33194} It shows no significant binding against a panel of 442 other kinases when tested at a concentration of 10 µM and exhibits high oral efficacy in mouse cancer models.{33193} AZD 8186 inhibits growth of a range of cell lines, with preferential activity in cells with PTEN mutation or deficiency, and inhibits growth of prostate and triple negative breast cancer tumors in vivo, both as a single agent and in combination with docetaxel (Item No. 11637).{33194}
Brand:CaymanSKU:-Available on backorder
AZD 8330 is a selective allosteric inhibitor of MEK1/2 (IC50 = 7 nM). It blocks phosphorylation of ERK1/2 and inhibits proliferation of certain cancer cells.{32893} AZD 8330 is orally bioavailable, inhibits ERK phosphorylation in vivo, and reduces tumor growth in a Calu-6 nude rat xenograft model.{32894}
Brand:CaymanSKU:11588 - 1 mgAvailable on backorder
AZD 8330 is a selective allosteric inhibitor of MEK1/2 (IC50 = 7 nM). It blocks phosphorylation of ERK1/2 and inhibits proliferation of certain cancer cells.{32893} AZD 8330 is orally bioavailable, inhibits ERK phosphorylation in vivo, and reduces tumor growth in a Calu-6 nude rat xenograft model.{32894}
Brand:CaymanSKU:11588 - 10 mgAvailable on backorder
AZD 8330 is a selective allosteric inhibitor of MEK1/2 (IC50 = 7 nM). It blocks phosphorylation of ERK1/2 and inhibits proliferation of certain cancer cells.{32893} AZD 8330 is orally bioavailable, inhibits ERK phosphorylation in vivo, and reduces tumor growth in a Calu-6 nude rat xenograft model.{32894}
Brand:CaymanSKU:11588 - 5 mgAvailable on backorder
AZD 8330 is a selective allosteric inhibitor of MEK1/2 (IC50 = 7 nM). It blocks phosphorylation of ERK1/2 and inhibits proliferation of certain cancer cells.{32893} AZD 8330 is orally bioavailable, inhibits ERK phosphorylation in vivo, and reduces tumor growth in a Calu-6 nude rat xenograft model.{32894}
Brand:CaymanSKU:11588 - 50 mgAvailable on backorder
AZD 8835 is an inhibitor of PI3Kα and PI3Kδ (IC50s = 6.2 and 5.7 nM, respectively).{48678} It is selective for PI3Kα and PI3Kδ over PI3Kβ and PI3Kγ (IC50s = 431 and 90 nM, respectively). AZD 8835 inhibits Akt phosphorylation in PIK3CA constitutively active mutant BT474 cells and Jeko-1 B cells that express endogenous PI3Kδ (IC50s = 57 and 49 nM, respectively). In vivo, AZD 8835 (25 mg/kg) reduces tumor growth and Akt phosphorylation in a SKOV3 mouse xenograft model. It also increases the activity of CD8+ effector T cells and reduces tumor growth in a C26 mouse syngeneic tumor model.{48679}
Brand:CaymanSKU:29166 - 1 mgAvailable on backorder
AZD 8835 is an inhibitor of PI3Kα and PI3Kδ (IC50s = 6.2 and 5.7 nM, respectively).{48678} It is selective for PI3Kα and PI3Kδ over PI3Kβ and PI3Kγ (IC50s = 431 and 90 nM, respectively). AZD 8835 inhibits Akt phosphorylation in PIK3CA constitutively active mutant BT474 cells and Jeko-1 B cells that express endogenous PI3Kδ (IC50s = 57 and 49 nM, respectively). In vivo, AZD 8835 (25 mg/kg) reduces tumor growth and Akt phosphorylation in a SKOV3 mouse xenograft model. It also increases the activity of CD8+ effector T cells and reduces tumor growth in a C26 mouse syngeneic tumor model.{48679}
Brand:CaymanSKU:29166 - 10 mgAvailable on backorder
AZD 8835 is an inhibitor of PI3Kα and PI3Kδ (IC50s = 6.2 and 5.7 nM, respectively).{48678} It is selective for PI3Kα and PI3Kδ over PI3Kβ and PI3Kγ (IC50s = 431 and 90 nM, respectively). AZD 8835 inhibits Akt phosphorylation in PIK3CA constitutively active mutant BT474 cells and Jeko-1 B cells that express endogenous PI3Kδ (IC50s = 57 and 49 nM, respectively). In vivo, AZD 8835 (25 mg/kg) reduces tumor growth and Akt phosphorylation in a SKOV3 mouse xenograft model. It also increases the activity of CD8+ effector T cells and reduces tumor growth in a C26 mouse syngeneic tumor model.{48679}
Brand:CaymanSKU:29166 - 25 mgAvailable on backorder
AZD 8835 is an inhibitor of PI3Kα and PI3Kδ (IC50s = 6.2 and 5.7 nM, respectively).{48678} It is selective for PI3Kα and PI3Kδ over PI3Kβ and PI3Kγ (IC50s = 431 and 90 nM, respectively). AZD 8835 inhibits Akt phosphorylation in PIK3CA constitutively active mutant BT474 cells and Jeko-1 B cells that express endogenous PI3Kδ (IC50s = 57 and 49 nM, respectively). In vivo, AZD 8835 (25 mg/kg) reduces tumor growth and Akt phosphorylation in a SKOV3 mouse xenograft model. It also increases the activity of CD8+ effector T cells and reduces tumor growth in a C26 mouse syngeneic tumor model.{48679}
Brand:CaymanSKU:29166 - 5 mgAvailable on backorder
AZD 8931 is a reversible inhibitor of the receptor tyrosine kinases ErbB1/EGFR, ErbB2/HER2, and ErbB3/HER3 (IC50s = 4, 3, and 4 nM, respectively, for autophosphorylation).{42033} In vitro, AZD 8931 (0.01, 0.1, and 1 µM) suppresses cell growth and induces apoptosis in SUM149 and FC-IBC-02 human breast cancer cell lines.{42034} In vivo, AZD 8931 (6.25-50 mg/kg) inhibits tumor growth in BT474c, Calu-3, LoVo, FaDu, and PC-9 mouse xenograft models.{42033} When administered in combination with paclitaxel (Item No. 10461), AZD 8931 inhibits inflammatory breast cancer tumor growth in a mouse xenograft model when administered at a dose of 25 mg/kg per day.{42034}
Brand:CaymanSKU:24196 - 1 mgAvailable on backorder
AZD 8931 is a reversible inhibitor of the receptor tyrosine kinases ErbB1/EGFR, ErbB2/HER2, and ErbB3/HER3 (IC50s = 4, 3, and 4 nM, respectively, for autophosphorylation).{42033} In vitro, AZD 8931 (0.01, 0.1, and 1 µM) suppresses cell growth and induces apoptosis in SUM149 and FC-IBC-02 human breast cancer cell lines.{42034} In vivo, AZD 8931 (6.25-50 mg/kg) inhibits tumor growth in BT474c, Calu-3, LoVo, FaDu, and PC-9 mouse xenograft models.{42033} When administered in combination with paclitaxel (Item No. 10461), AZD 8931 inhibits inflammatory breast cancer tumor growth in a mouse xenograft model when administered at a dose of 25 mg/kg per day.{42034}
Brand:CaymanSKU:24196 - 10 mgAvailable on backorder
AZD 8931 is a reversible inhibitor of the receptor tyrosine kinases ErbB1/EGFR, ErbB2/HER2, and ErbB3/HER3 (IC50s = 4, 3, and 4 nM, respectively, for autophosphorylation).{42033} In vitro, AZD 8931 (0.01, 0.1, and 1 µM) suppresses cell growth and induces apoptosis in SUM149 and FC-IBC-02 human breast cancer cell lines.{42034} In vivo, AZD 8931 (6.25-50 mg/kg) inhibits tumor growth in BT474c, Calu-3, LoVo, FaDu, and PC-9 mouse xenograft models.{42033} When administered in combination with paclitaxel (Item No. 10461), AZD 8931 inhibits inflammatory breast cancer tumor growth in a mouse xenograft model when administered at a dose of 25 mg/kg per day.{42034}
Brand:CaymanSKU:24196 - 25 mgAvailable on backorder
AZD 8931 is a reversible inhibitor of the receptor tyrosine kinases ErbB1/EGFR, ErbB2/HER2, and ErbB3/HER3 (IC50s = 4, 3, and 4 nM, respectively, for autophosphorylation).{42033} In vitro, AZD 8931 (0.01, 0.1, and 1 µM) suppresses cell growth and induces apoptosis in SUM149 and FC-IBC-02 human breast cancer cell lines.{42034} In vivo, AZD 8931 (6.25-50 mg/kg) inhibits tumor growth in BT474c, Calu-3, LoVo, FaDu, and PC-9 mouse xenograft models.{42033} When administered in combination with paclitaxel (Item No. 10461), AZD 8931 inhibits inflammatory breast cancer tumor growth in a mouse xenograft model when administered at a dose of 25 mg/kg per day.{42034}
Brand:CaymanSKU:24196 - 5 mgAvailable on backorder
AZD 9272 is a brain-penetrant negative allosteric modulator of metabotropic glutamate receptor 5 (mGluR5; IC50 = 7.6 nM in a FLIPR calcium mobilization assay).{45717} It is selective for mGluR5 over mGluR1-4 and 6-8 in a FLIPR calcium mobilization assay (IC50s = >30 µM) and a panel of 134 receptors, ion channels, nuclear hormone receptors, transporters, and enzymes at 10 µM in radioligand binding assays.
Brand:CaymanSKU:29717 - 10 mgAvailable on backorder
AZD 9272 is a brain-penetrant negative allosteric modulator of metabotropic glutamate receptor 5 (mGluR5; IC50 = 7.6 nM in a FLIPR calcium mobilization assay).{45717} It is selective for mGluR5 over mGluR1-4 and 6-8 in a FLIPR calcium mobilization assay (IC50s = >30 µM) and a panel of 134 receptors, ion channels, nuclear hormone receptors, transporters, and enzymes at 10 µM in radioligand binding assays.
Brand:CaymanSKU:29717 - 25 mgAvailable on backorder
AZD 9272 is a brain-penetrant negative allosteric modulator of metabotropic glutamate receptor 5 (mGluR5; IC50 = 7.6 nM in a FLIPR calcium mobilization assay).{45717} It is selective for mGluR5 over mGluR1-4 and 6-8 in a FLIPR calcium mobilization assay (IC50s = >30 µM) and a panel of 134 receptors, ion channels, nuclear hormone receptors, transporters, and enzymes at 10 µM in radioligand binding assays.
Brand:CaymanSKU:29717 - 5 mgAvailable on backorder
AZD 9291 is an irreversible inhibitor of epidermal growth factor receptor (EGFR) sensitizing and T790M resistance mutations (IC50s = 15-17 nM) while sparing the wild-type form of the receptor (IC50 = 480 nM).{27820} It binds the related IGF1R and hERG receptors with significantly reduced potency (IC50s = 2.9 and 16.2 µM, respectively).{27820} AZD 9291 has been shown to inhibit tumor growth in a xenograft mouse model at oral doses of 5-10 mg/kg and has been tested clinically in patients with advanced EGFR mutant non-small-cell lung cancer.{27820}
Brand:CaymanSKU:- AZD 9291 is an irreversible inhibitor of epidermal growth factor receptor (EGFR) sensitizing and T790M resistance mutations (IC50s = 15-17 nM) while sparing the wild-type form of the receptor (IC50 = 480 nM).{27820} It binds the related IGF1R and hERG receptors with significantly reduced potency (IC50s = 2.9 and 16.2 µM, respectively).{27820} AZD 9291 has been shown to inhibit tumor growth in a xenograft mouse model at oral doses of 5-10 mg/kg and has been tested clinically in patients with advanced EGFR mutant non-small-cell lung cancer.{27820}
Brand:CaymanSKU:- AZD 9291 is an irreversible inhibitor of epidermal growth factor receptor (EGFR) sensitizing and T790M resistance mutations (IC50s = 15-17 nM) while sparing the wild-type form of the receptor (IC50 = 480 nM).{27820} It binds the related IGF1R and hERG receptors with significantly reduced potency (IC50s = 2.9 and 16.2 µM, respectively).{27820} AZD 9291 has been shown to inhibit tumor growth in a xenograft mouse model at oral doses of 5-10 mg/kg and has been tested clinically in patients with advanced EGFR mutant non-small-cell lung cancer.{27820}
Brand:CaymanSKU:- AZD 9291 is an irreversible inhibitor of epidermal growth factor receptor (EGFR) sensitizing and T790M resistance mutations (IC50s = 15-17 nM) while sparing the wild-type form of the receptor (IC50 = 480 nM).{27820} It binds the related IGF1R and hERG receptors with significantly reduced potency (IC50s = 2.9 and 16.2 µM, respectively).{27820} AZD 9291 has been shown to inhibit tumor growth in a xenograft mouse model at oral doses of 5-10 mg/kg and has been tested clinically in patients with advanced EGFR mutant non-small-cell lung cancer.{27820}
Brand:CaymanSKU:-
AZD 9496 is a potent and selective estrogen receptor downregulator (SERD) with an IC50 value of 0.138 nM for estrogen receptor α (ERα) downregulation.{39174} It is selective for ERα compared to other nuclear hormone receptors with IC50 values of 0.0008, 0.54, 9.2, and 30 μM for ERα, progesterone receptor (PR), glucocorticoid receptor (GR), and androgen receptor (AR), respectively. AZD 9496 decreases ERα activity (IC50 = 0.282 nM), measured via quantification of downstream PR activity, and reduces proliferation of MCF-7 breast cancer cells (IC50 = 0.0398 nM). It also inhibits MCF-7 xenograft growth in mice in a dose-dependent manner. AZD 9496 is orally bioavailable and formulations containing it are under investigation in clinical trials for treatment of ER positive breast cancer.
Brand:CaymanSKU:21805 -Out of stock
AZD 9496 is a potent and selective estrogen receptor downregulator (SERD) with an IC50 value of 0.138 nM for estrogen receptor α (ERα) downregulation.{39174} It is selective for ERα compared to other nuclear hormone receptors with IC50 values of 0.0008, 0.54, 9.2, and 30 μM for ERα, progesterone receptor (PR), glucocorticoid receptor (GR), and androgen receptor (AR), respectively. AZD 9496 decreases ERα activity (IC50 = 0.282 nM), measured via quantification of downstream PR activity, and reduces proliferation of MCF-7 breast cancer cells (IC50 = 0.0398 nM). It also inhibits MCF-7 xenograft growth in mice in a dose-dependent manner. AZD 9496 is orally bioavailable and formulations containing it are under investigation in clinical trials for treatment of ER positive breast cancer.
Brand:CaymanSKU:21805 -Out of stock
AZD 9496 is a potent and selective estrogen receptor downregulator (SERD) with an IC50 value of 0.138 nM for estrogen receptor α (ERα) downregulation.{39174} It is selective for ERα compared to other nuclear hormone receptors with IC50 values of 0.0008, 0.54, 9.2, and 30 μM for ERα, progesterone receptor (PR), glucocorticoid receptor (GR), and androgen receptor (AR), respectively. AZD 9496 decreases ERα activity (IC50 = 0.282 nM), measured via quantification of downstream PR activity, and reduces proliferation of MCF-7 breast cancer cells (IC50 = 0.0398 nM). It also inhibits MCF-7 xenograft growth in mice in a dose-dependent manner. AZD 9496 is orally bioavailable and formulations containing it are under investigation in clinical trials for treatment of ER positive breast cancer.
Brand:CaymanSKU:21805 -Out of stock
AZD 9496 is a potent and selective estrogen receptor downregulator (SERD) with an IC50 value of 0.138 nM for estrogen receptor α (ERα) downregulation.{39174} It is selective for ERα compared to other nuclear hormone receptors with IC50 values of 0.0008, 0.54, 9.2, and 30 μM for ERα, progesterone receptor (PR), glucocorticoid receptor (GR), and androgen receptor (AR), respectively. AZD 9496 decreases ERα activity (IC50 = 0.282 nM), measured via quantification of downstream PR activity, and reduces proliferation of MCF-7 breast cancer cells (IC50 = 0.0398 nM). It also inhibits MCF-7 xenograft growth in mice in a dose-dependent manner. AZD 9496 is orally bioavailable and formulations containing it are under investigation in clinical trials for treatment of ER positive breast cancer.
Brand:CaymanSKU:21805 -Out of stock
AZD 9668 is an orally bioavailable inhibitor of neutrophil elastase (IC50 = 12 nM for the human enzyme).{42559} It is greater than 600-fold selective for neutrophil elastase over other serine proteases, including human proteinase-3 and cathepsin G, bovine trypsin and chymotrypsin, and porcine pancreatic elastase. AZD 9668 inhibits neutrophil elastase activity in zymosan-stimulated isolated whole blood and in cell-associated assays (IC50s = 46 and 48 nM, respectively). It decreases the number of neutrophils in bronchoalveolar lavage fluid (BALF) in a mouse model of smoke-induced airway inflammation when administered at a dose of 6 mg/kg. AZD 9668 also prevents airspace enlargement and small airway remodeling in a guinea pig model of chronic smoke-induced inflammation and emphysema.
Brand:CaymanSKU:26083 - 1 mgAvailable on backorder
AZD 9668 is an orally bioavailable inhibitor of neutrophil elastase (IC50 = 12 nM for the human enzyme).{42559} It is greater than 600-fold selective for neutrophil elastase over other serine proteases, including human proteinase-3 and cathepsin G, bovine trypsin and chymotrypsin, and porcine pancreatic elastase. AZD 9668 inhibits neutrophil elastase activity in zymosan-stimulated isolated whole blood and in cell-associated assays (IC50s = 46 and 48 nM, respectively). It decreases the number of neutrophils in bronchoalveolar lavage fluid (BALF) in a mouse model of smoke-induced airway inflammation when administered at a dose of 6 mg/kg. AZD 9668 also prevents airspace enlargement and small airway remodeling in a guinea pig model of chronic smoke-induced inflammation and emphysema.
Brand:CaymanSKU:26083 - 10 mgAvailable on backorder
AZD 9668 is an orally bioavailable inhibitor of neutrophil elastase (IC50 = 12 nM for the human enzyme).{42559} It is greater than 600-fold selective for neutrophil elastase over other serine proteases, including human proteinase-3 and cathepsin G, bovine trypsin and chymotrypsin, and porcine pancreatic elastase. AZD 9668 inhibits neutrophil elastase activity in zymosan-stimulated isolated whole blood and in cell-associated assays (IC50s = 46 and 48 nM, respectively). It decreases the number of neutrophils in bronchoalveolar lavage fluid (BALF) in a mouse model of smoke-induced airway inflammation when administered at a dose of 6 mg/kg. AZD 9668 also prevents airspace enlargement and small airway remodeling in a guinea pig model of chronic smoke-induced inflammation and emphysema.
Brand:CaymanSKU:26083 - 25 mgAvailable on backorder
AZD 9668 is an orally bioavailable inhibitor of neutrophil elastase (IC50 = 12 nM for the human enzyme).{42559} It is greater than 600-fold selective for neutrophil elastase over other serine proteases, including human proteinase-3 and cathepsin G, bovine trypsin and chymotrypsin, and porcine pancreatic elastase. AZD 9668 inhibits neutrophil elastase activity in zymosan-stimulated isolated whole blood and in cell-associated assays (IC50s = 46 and 48 nM, respectively). It decreases the number of neutrophils in bronchoalveolar lavage fluid (BALF) in a mouse model of smoke-induced airway inflammation when administered at a dose of 6 mg/kg. AZD 9668 also prevents airspace enlargement and small airway remodeling in a guinea pig model of chronic smoke-induced inflammation and emphysema.
Brand:CaymanSKU:26083 - 5 mgAvailable on backorder
Janus-associated kinases (JAKs) are cytoplasmic tyrosine kinases that are required for activating the signaling of certain cytokines and growth factor receptors. Many myeloproliferative diseases have been linked to a mutation in JAK2 where a switch from valine to phenylalanine occurs at the 617 position (V617F).{27171} AZD1480 is a potent JAK2 inhibitor that blocks signaling (IC50 = 58 nM at 5 mM ATP) and proliferation of JAK2-expressing cell lines (GI50 = 60 nM).{29735,18888} It is selective for JAK2 over other JAK family members as well as a panel of related kinases.{18888} AZD1480 also inhibits the growth of cells expressing the V617F mutant of JAK2 (GI50 = 60 nM).{18888} It reversibly blocks JAK2-mediated phosphorylation of STAT3 and STAT5.{18888} AZD1480 displays good pharmacokinetics in vivo, inhibits STAT3 and STAT5 activation in vivo, and suppresses tumorigenesis in mouse xenografts harboring constitutive STAT3 activity.{29735,18888} In addition to suppressing myeloma cell growth and survival, AZD1480 reduces angiogenesis and metastasis in vitro and in human xenograft tumor models.{29736,29737}
Brand:CaymanSKU:10702 - 1 mgAvailable on backorder
Janus-associated kinases (JAKs) are cytoplasmic tyrosine kinases that are required for activating the signaling of certain cytokines and growth factor receptors. Many myeloproliferative diseases have been linked to a mutation in JAK2 where a switch from valine to phenylalanine occurs at the 617 position (V617F).{27171} AZD1480 is a potent JAK2 inhibitor that blocks signaling (IC50 = 58 nM at 5 mM ATP) and proliferation of JAK2-expressing cell lines (GI50 = 60 nM).{29735,18888} It is selective for JAK2 over other JAK family members as well as a panel of related kinases.{18888} AZD1480 also inhibits the growth of cells expressing the V617F mutant of JAK2 (GI50 = 60 nM).{18888} It reversibly blocks JAK2-mediated phosphorylation of STAT3 and STAT5.{18888} AZD1480 displays good pharmacokinetics in vivo, inhibits STAT3 and STAT5 activation in vivo, and suppresses tumorigenesis in mouse xenografts harboring constitutive STAT3 activity.{29735,18888} In addition to suppressing myeloma cell growth and survival, AZD1480 reduces angiogenesis and metastasis in vitro and in human xenograft tumor models.{29736,29737}
Brand:CaymanSKU:10702 - 10 mgAvailable on backorder
Janus-associated kinases (JAKs) are cytoplasmic tyrosine kinases that are required for activating the signaling of certain cytokines and growth factor receptors. Many myeloproliferative diseases have been linked to a mutation in JAK2 where a switch from valine to phenylalanine occurs at the 617 position (V617F).{27171} AZD1480 is a potent JAK2 inhibitor that blocks signaling (IC50 = 58 nM at 5 mM ATP) and proliferation of JAK2-expressing cell lines (GI50 = 60 nM).{29735,18888} It is selective for JAK2 over other JAK family members as well as a panel of related kinases.{18888} AZD1480 also inhibits the growth of cells expressing the V617F mutant of JAK2 (GI50 = 60 nM).{18888} It reversibly blocks JAK2-mediated phosphorylation of STAT3 and STAT5.{18888} AZD1480 displays good pharmacokinetics in vivo, inhibits STAT3 and STAT5 activation in vivo, and suppresses tumorigenesis in mouse xenografts harboring constitutive STAT3 activity.{29735,18888} In addition to suppressing myeloma cell growth and survival, AZD1480 reduces angiogenesis and metastasis in vitro and in human xenograft tumor models.{29736,29737}
Brand:CaymanSKU:10702 - 5 mgAvailable on backorder
Janus-associated kinases (JAKs) are cytoplasmic tyrosine kinases that are required for activating the signaling of certain cytokines and growth factor receptors. Many myeloproliferative diseases have been linked to a mutation in JAK2 where a switch from valine to phenylalanine occurs at the 617 position (V617F).{27171} AZD1480 is a potent JAK2 inhibitor that blocks signaling (IC50 = 58 nM at 5 mM ATP) and proliferation of JAK2-expressing cell lines (GI50 = 60 nM).{29735,18888} It is selective for JAK2 over other JAK family members as well as a panel of related kinases.{18888} AZD1480 also inhibits the growth of cells expressing the V617F mutant of JAK2 (GI50 = 60 nM).{18888} It reversibly blocks JAK2-mediated phosphorylation of STAT3 and STAT5.{18888} AZD1480 displays good pharmacokinetics in vivo, inhibits STAT3 and STAT5 activation in vivo, and suppresses tumorigenesis in mouse xenografts harboring constitutive STAT3 activity.{29735,18888} In addition to suppressing myeloma cell growth and survival, AZD1480 reduces angiogenesis and metastasis in vitro and in human xenograft tumor models.{29736,29737}
Brand:CaymanSKU:10702 - 50 mgAvailable on backorder
AZD3839 is an inhibitor of beta-secretase 1 (BACE1).{48539,48540} It selectively binds to BACE1 over BACE2 (Kis = 26.1 and 372.4 nM, respectively, for the human enzymes).{48539} It also inhibits human ether-a-go-go-related gene (hERG) potassium channels expressed in CHO cells (IC50 = 4.8 μM).{48540} AZD3839 decreases amyloid-β (Aβ) secretion from mouse Neuro2a neuroblastoma cells and primary neurons (IC50s = 32.2 and 50.9 nM, respectively).{48539} It dose- and time-dependently decreases Aβ levels in the plasma and brain of mice and guinea pigs. AZD3839 also decreases Aβ in the cerebrospinal fluid (CSF) of cynomolgus monkeys when administered at a dose of 20 μmol/kg.
Brand:CaymanSKU:28388 - 1 mgAvailable on backorder
AZD3839 is an inhibitor of beta-secretase 1 (BACE1).{48539,48540} It selectively binds to BACE1 over BACE2 (Kis = 26.1 and 372.4 nM, respectively, for the human enzymes).{48539} It also inhibits human ether-a-go-go-related gene (hERG) potassium channels expressed in CHO cells (IC50 = 4.8 μM).{48540} AZD3839 decreases amyloid-β (Aβ) secretion from mouse Neuro2a neuroblastoma cells and primary neurons (IC50s = 32.2 and 50.9 nM, respectively).{48539} It dose- and time-dependently decreases Aβ levels in the plasma and brain of mice and guinea pigs. AZD3839 also decreases Aβ in the cerebrospinal fluid (CSF) of cynomolgus monkeys when administered at a dose of 20 μmol/kg.
Brand:CaymanSKU:28388 - 10 mgAvailable on backorder
AZD3839 is an inhibitor of beta-secretase 1 (BACE1).{48539,48540} It selectively binds to BACE1 over BACE2 (Kis = 26.1 and 372.4 nM, respectively, for the human enzymes).{48539} It also inhibits human ether-a-go-go-related gene (hERG) potassium channels expressed in CHO cells (IC50 = 4.8 μM).{48540} AZD3839 decreases amyloid-β (Aβ) secretion from mouse Neuro2a neuroblastoma cells and primary neurons (IC50s = 32.2 and 50.9 nM, respectively).{48539} It dose- and time-dependently decreases Aβ levels in the plasma and brain of mice and guinea pigs. AZD3839 also decreases Aβ in the cerebrospinal fluid (CSF) of cynomolgus monkeys when administered at a dose of 20 μmol/kg.
Brand:CaymanSKU:28388 - 25 mgAvailable on backorder
AZD3839 is an inhibitor of beta-secretase 1 (BACE1).{48539,48540} It selectively binds to BACE1 over BACE2 (Kis = 26.1 and 372.4 nM, respectively, for the human enzymes).{48539} It also inhibits human ether-a-go-go-related gene (hERG) potassium channels expressed in CHO cells (IC50 = 4.8 μM).{48540} AZD3839 decreases amyloid-β (Aβ) secretion from mouse Neuro2a neuroblastoma cells and primary neurons (IC50s = 32.2 and 50.9 nM, respectively).{48539} It dose- and time-dependently decreases Aβ levels in the plasma and brain of mice and guinea pigs. AZD3839 also decreases Aβ in the cerebrospinal fluid (CSF) of cynomolgus monkeys when administered at a dose of 20 μmol/kg.
Brand:CaymanSKU:28388 - 5 mgAvailable on backorder
Phosphatidylinositol 3-kinase (PI3K) catalyzes the phosphorylation of the 3′ hydroxyl position of PIs to produce the second messengers PtdIns-(3,4)-P2 and PtdIns-(3,4,5)-P3.{8039,12235,13740} PI3Kα, β, and δ are class 1A enzymes composed of p110 and p85 subunits, whereas PI3Kγ is a class 1B PI3K composed of a p110 catalytic subunit and a p101 or p84 regulatory subunit.{14518} AZD6482 is a PI3K inhibitor that targets the β isoform more potently than PI3Kδ, PI3Kγ, or PI3Kα (IC50s = 0.69, 13.6, 47.8, and 136 nM, respectively).{29907} It displays 80-fold selectivity for PI3Kβ over PI3k-C2 and DNA-PK and more than 1,000-fold over other PI3K-related kinases.{29907} AZD6482 blocks Akt signaling and tumor growth in a large number of cancer cell lines, including those that are dependent on PI3Kβ activation or PTEN loss.{29907,29910,29908} AZD6482 (20 mg/kg, i.p.) suppresses the growth of PTEN-deficient xenograft tumors in mice.{29907} It also produces an anti-thrombotic effect in dogs without an increase in bleeding time or blood loss.{29909}
Brand:CaymanSKU:- Phosphatidylinositol 3-kinase (PI3K) catalyzes the phosphorylation of the 3′ hydroxyl position of PIs to produce the second messengers PtdIns-(3,4)-P2 and PtdIns-(3,4,5)-P3.{8039,12235,13740} PI3Kα, β, and δ are class 1A enzymes composed of p110 and p85 subunits, whereas PI3Kγ is a class 1B PI3K composed of a p110 catalytic subunit and a p101 or p84 regulatory subunit.{14518} AZD6482 is a PI3K inhibitor that targets the β isoform more potently than PI3Kδ, PI3Kγ, or PI3Kα (IC50s = 0.69, 13.6, 47.8, and 136 nM, respectively).{29907} It displays 80-fold selectivity for PI3Kβ over PI3k-C2 and DNA-PK and more than 1,000-fold over other PI3K-related kinases.{29907} AZD6482 blocks Akt signaling and tumor growth in a large number of cancer cell lines, including those that are dependent on PI3Kβ activation or PTEN loss.{29907,29910,29908} AZD6482 (20 mg/kg, i.p.) suppresses the growth of PTEN-deficient xenograft tumors in mice.{29907} It also produces an anti-thrombotic effect in dogs without an increase in bleeding time or blood loss.{29909}
Brand:CaymanSKU:- Phosphatidylinositol 3-kinase (PI3K) catalyzes the phosphorylation of the 3′ hydroxyl position of PIs to produce the second messengers PtdIns-(3,4)-P2 and PtdIns-(3,4,5)-P3.{8039,12235,13740} PI3Kα, β, and δ are class 1A enzymes composed of p110 and p85 subunits, whereas PI3Kγ is a class 1B PI3K composed of a p110 catalytic subunit and a p101 or p84 regulatory subunit.{14518} AZD6482 is a PI3K inhibitor that targets the β isoform more potently than PI3Kδ, PI3Kγ, or PI3Kα (IC50s = 0.69, 13.6, 47.8, and 136 nM, respectively).{29907} It displays 80-fold selectivity for PI3Kβ over PI3k-C2 and DNA-PK and more than 1,000-fold over other PI3K-related kinases.{29907} AZD6482 blocks Akt signaling and tumor growth in a large number of cancer cell lines, including those that are dependent on PI3Kβ activation or PTEN loss.{29907,29910,29908} AZD6482 (20 mg/kg, i.p.) suppresses the growth of PTEN-deficient xenograft tumors in mice.{29907} It also produces an anti-thrombotic effect in dogs without an increase in bleeding time or blood loss.{29909}
Brand:CaymanSKU:- Phosphatidylinositol 3-kinase (PI3K) catalyzes the phosphorylation of the 3′ hydroxyl position of PIs to produce the second messengers PtdIns-(3,4)-P2 and PtdIns-(3,4,5)-P3.{8039,12235,13740} PI3Kα, β, and δ are class 1A enzymes composed of p110 and p85 subunits, whereas PI3Kγ is a class 1B PI3K composed of a p110 catalytic subunit and a p101 or p84 regulatory subunit.{14518} AZD6482 is a PI3K inhibitor that targets the β isoform more potently than PI3Kδ, PI3Kγ, or PI3Kα (IC50s = 0.69, 13.6, 47.8, and 136 nM, respectively).{29907} It displays 80-fold selectivity for PI3Kβ over PI3k-C2 and DNA-PK and more than 1,000-fold over other PI3K-related kinases.{29907} AZD6482 blocks Akt signaling and tumor growth in a large number of cancer cell lines, including those that are dependent on PI3Kβ activation or PTEN loss.{29907,29910,29908} AZD6482 (20 mg/kg, i.p.) suppresses the growth of PTEN-deficient xenograft tumors in mice.{29907} It also produces an anti-thrombotic effect in dogs without an increase in bleeding time or blood loss.{29909}
Brand:CaymanSKU:-
Azelaic acid is a naturally occurring and saturated dicarboxylic acid with diverse biological activities.{38830,38831,38832,38833,38834} It is a competitive inhibitor of tyrosinase, NADH dehydrogenase, succinic dehydrogenase, and reduced ubiquitinone:cytochrome C oxidoreductase in vitro.{38830,38831} Azelaic acid inhibits the growth and colony formation of B16 murine as well as HMB2 and SK32 human melanoma cells in a concentration-dependent manner but has no effect on CHO cells.{38832} It decreases DNA synthesis, induces mitochondrial damage and dilation of the rough endoplasmic reticulum (RER), and reduces growth of mouse keratinocytes in a dose- and time-dependent manner.{38833} Azelaic acid is bacteriostatic against S. epidermidis, S. aureus, S. capitis, P. acnes, P. avidum, P. mirabilis, and C. albicans in vitro (MICs = 0.03-0.25 M).{38834} Formulations containing azelaic acid have been used in the treatment of acne and hyperpigmentation disorders.
Brand:CaymanSKU:23977 - 100 gAvailable on backorder
Azelaic acid is a naturally occurring and saturated dicarboxylic acid with diverse biological activities.{38830,38831,38832,38833,38834} It is a competitive inhibitor of tyrosinase, NADH dehydrogenase, succinic dehydrogenase, and reduced ubiquitinone:cytochrome C oxidoreductase in vitro.{38830,38831} Azelaic acid inhibits the growth and colony formation of B16 murine as well as HMB2 and SK32 human melanoma cells in a concentration-dependent manner but has no effect on CHO cells.{38832} It decreases DNA synthesis, induces mitochondrial damage and dilation of the rough endoplasmic reticulum (RER), and reduces growth of mouse keratinocytes in a dose- and time-dependent manner.{38833} Azelaic acid is bacteriostatic against S. epidermidis, S. aureus, S. capitis, P. acnes, P. avidum, P. mirabilis, and C. albicans in vitro (MICs = 0.03-0.25 M).{38834} Formulations containing azelaic acid have been used in the treatment of acne and hyperpigmentation disorders.
Brand:CaymanSKU:23977 - 25 gAvailable on backorder
Azelaic acid is a naturally occurring and saturated dicarboxylic acid with diverse biological activities.{38830,38831,38832,38833,38834} It is a competitive inhibitor of tyrosinase, NADH dehydrogenase, succinic dehydrogenase, and reduced ubiquitinone:cytochrome C oxidoreductase in vitro.{38830,38831} Azelaic acid inhibits the growth and colony formation of B16 murine as well as HMB2 and SK32 human melanoma cells in a concentration-dependent manner but has no effect on CHO cells.{38832} It decreases DNA synthesis, induces mitochondrial damage and dilation of the rough endoplasmic reticulum (RER), and reduces growth of mouse keratinocytes in a dose- and time-dependent manner.{38833} Azelaic acid is bacteriostatic against S. epidermidis, S. aureus, S. capitis, P. acnes, P. avidum, P. mirabilis, and C. albicans in vitro (MICs = 0.03-0.25 M).{38834} Formulations containing azelaic acid have been used in the treatment of acne and hyperpigmentation disorders.
Brand:CaymanSKU:23977 - 250 gAvailable on backorder
Azelaic acid is a naturally occurring and saturated dicarboxylic acid with diverse biological activities.{38830,38831,38832,38833,38834} It is a competitive inhibitor of tyrosinase, NADH dehydrogenase, succinic dehydrogenase, and reduced ubiquitinone:cytochrome C oxidoreductase in vitro.{38830,38831} Azelaic acid inhibits the growth and colony formation of B16 murine as well as HMB2 and SK32 human melanoma cells in a concentration-dependent manner but has no effect on CHO cells.{38832} It decreases DNA synthesis, induces mitochondrial damage and dilation of the rough endoplasmic reticulum (RER), and reduces growth of mouse keratinocytes in a dose- and time-dependent manner.{38833} Azelaic acid is bacteriostatic against S. epidermidis, S. aureus, S. capitis, P. acnes, P. avidum, P. mirabilis, and C. albicans in vitro (MICs = 0.03-0.25 M).{38834} Formulations containing azelaic acid have been used in the treatment of acne and hyperpigmentation disorders.
Brand:CaymanSKU:23977 - 50 gAvailable on backorder
Oxidized low-density lipoprotein (oxLDL) particles contain low molecular weight species which promote the differentiation of monocytes via the nuclear receptor PPARγ.{8499} One of these substances was recently isolated and purified from oxLDL, and identified as azelaoyl PAF.{8953} Azelaoyl PAF is a potent PPARγ agonist which competes for the thiazolidinedione binding site. Azelaoyl PAF is more potent than 15-deoxy-Δ12,14-prostaglandin J2, and equipotent with rosiglitazone as a ligand for this receptor.{8953}
Brand:CaymanSKU:60924 - 1 mgAvailable on backorder
Oxidized low-density lipoprotein (oxLDL) particles contain low molecular weight species which promote the differentiation of monocytes via the nuclear receptor PPARγ.{8499} One of these substances was recently isolated and purified from oxLDL, and identified as azelaoyl PAF.{8953} Azelaoyl PAF is a potent PPARγ agonist which competes for the thiazolidinedione binding site. Azelaoyl PAF is more potent than 15-deoxy-Δ12,14-prostaglandin J2, and equipotent with rosiglitazone as a ligand for this receptor.{8953}
Brand:CaymanSKU:60924 - 10 mgAvailable on backorder
Oxidized low-density lipoprotein (oxLDL) particles contain low molecular weight species which promote the differentiation of monocytes via the nuclear receptor PPARγ.{8499} One of these substances was recently isolated and purified from oxLDL, and identified as azelaoyl PAF.{8953} Azelaoyl PAF is a potent PPARγ agonist which competes for the thiazolidinedione binding site. Azelaoyl PAF is more potent than 15-deoxy-Δ12,14-prostaglandin J2, and equipotent with rosiglitazone as a ligand for this receptor.{8953}
Brand:CaymanSKU:60924 - 5 mgAvailable on backorder
Oxidized low-density lipoprotein (oxLDL) particles contain low molecular weight species which promote the differentiation of monocytes via the nuclear receptor PPARγ.{8499} One of these substances was recently isolated and purified from oxLDL, and identified as azelaoyl PAF.{8953} Azelaoyl PAF is a potent PPARγ agonist which competes for the thiazolidinedione binding site. Azelaoyl PAF is more potent than 15-deoxy-Δ12,14-prostaglandin J2, and equipotent with rosiglitazone as a ligand for this receptor.{8953}
Brand:CaymanSKU:60924 - 500 µgAvailable on backorder
Azelastine is a second generation antihistamine that targets the histamine H1 receptor (Ki = 6.4 nM).{23214,31603} It displays a terminal half-life of 25 hours in man.{31603} Azelastine may be combined with the synthetic glucocorticoid fluticasone in certain formulations for the improvement of symptoms related to allergies.{32981}
Brand:CaymanSKU:20873 -Out of stock
Azelastine is a second generation antihistamine that targets the histamine H1 receptor (Ki = 6.4 nM).{23214,31603} It displays a terminal half-life of 25 hours in man.{31603} Azelastine may be combined with the synthetic glucocorticoid fluticasone in certain formulations for the improvement of symptoms related to allergies.{32981}
Brand:CaymanSKU:20873 -Out of stock
Azelastine is a second generation antihistamine that targets the histamine H1 receptor (Ki = 6.4 nM).{23214,31603} It displays a terminal half-life of 25 hours in man.{31603} Azelastine may be combined with the synthetic glucocorticoid fluticasone in certain formulations for the improvement of symptoms related to allergies.{32981}
Brand:CaymanSKU:20873 -Out of stock
Azeliragon is an orally bioavailable inhibitor of the receptor for advanced glycation endproducts (RAGE; Kd = 12.7 nM for human recombinant sRAGE), which transports amyloid-β (Aβ) from plasma into the CNS.{39734} It is selective for sRAGE over greater than 100 receptors and transporters in a screening assay. Azeliragon (0.3, 1, and 3 mg/kg per day) prevents brain deposition of Aβ (1-40) (Aβ40) and Aβ42 in the APP/SWE/LON transgenic mouse model of Alzheimer’s disease and increases plasma Aβ levels when administered for three months starting at 12 months of age. In the same treatment paradigm, it dose-dependently reduces memory impairments in the Morris water maze compared with untreated control mice, decreasing the latency and distance traveled to the platform. Azeliragon (10 mg/kg) also increases cerebral blood flow in the hippocampus and frontal cortex in tgAPP/SWE/LON mice greater than six months old.
Brand:CaymanSKU:24678 - 10 mgAvailable on backorder
Azeliragon is an orally bioavailable inhibitor of the receptor for advanced glycation endproducts (RAGE; Kd = 12.7 nM for human recombinant sRAGE), which transports amyloid-β (Aβ) from plasma into the CNS.{39734} It is selective for sRAGE over greater than 100 receptors and transporters in a screening assay. Azeliragon (0.3, 1, and 3 mg/kg per day) prevents brain deposition of Aβ (1-40) (Aβ40) and Aβ42 in the APP/SWE/LON transgenic mouse model of Alzheimer’s disease and increases plasma Aβ levels when administered for three months starting at 12 months of age. In the same treatment paradigm, it dose-dependently reduces memory impairments in the Morris water maze compared with untreated control mice, decreasing the latency and distance traveled to the platform. Azeliragon (10 mg/kg) also increases cerebral blood flow in the hippocampus and frontal cortex in tgAPP/SWE/LON mice greater than six months old.
Brand:CaymanSKU:24678 - 25 mgAvailable on backorder
Azeliragon is an orally bioavailable inhibitor of the receptor for advanced glycation endproducts (RAGE; Kd = 12.7 nM for human recombinant sRAGE), which transports amyloid-β (Aβ) from plasma into the CNS.{39734} It is selective for sRAGE over greater than 100 receptors and transporters in a screening assay. Azeliragon (0.3, 1, and 3 mg/kg per day) prevents brain deposition of Aβ (1-40) (Aβ40) and Aβ42 in the APP/SWE/LON transgenic mouse model of Alzheimer’s disease and increases plasma Aβ levels when administered for three months starting at 12 months of age. In the same treatment paradigm, it dose-dependently reduces memory impairments in the Morris water maze compared with untreated control mice, decreasing the latency and distance traveled to the platform. Azeliragon (10 mg/kg) also increases cerebral blood flow in the hippocampus and frontal cortex in tgAPP/SWE/LON mice greater than six months old.
Brand:CaymanSKU:24678 - 5 mgAvailable on backorder
Azelnidipine is a third generation, dihydropyridine L-type calcium channel blocker with a slow onset profile that displays long-lasting antihypertensive activity in hypertensive rat models compared to other L-type calcium channel blockers.{33379,33378}
Brand:CaymanSKU:21249 -Out of stock
Azelnidipine is a third generation, dihydropyridine L-type calcium channel blocker with a slow onset profile that displays long-lasting antihypertensive activity in hypertensive rat models compared to other L-type calcium channel blockers.{33379,33378}
Brand:CaymanSKU:21249 -Out of stock