Cayman
Showing 10951–11100 of 45550 results
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The two isoforms of glycogen synthase kinase 3, GSK3α and GSK3β, constitutively phosphorylate and inactivate glycogen synthase, preventing glycogen synthesis.{19045} They also phosphorylate proteins that are relevant to Alzheimer’s disease and osteogenesis.{25567,25565,25566} AZD 1080 is a potent, brain permeable inhibitor of GSK3α and GSK3β (Kis = 6.9 and 31 nM, respectively).{27257,27258} It shows >14-fold selectivity against several kinases, receptors, enzymes, and ion channels.{27257} AZD 1080 inhibits tau phosphorylation in cells.{27257} It shows good bioavailability after oral administration in vivo, inhibiting hippocampal tau phosphorylation and reversing cognitive deficits induced by the NMDA receptor antagonist (+)-MK-801 (Item No. 10009019).{27257} In humans, oral AZD 1080 inhibits GSK3 activity in peripheral blood lymphocytes following an initial delay in response.{27257}
Brand:CaymanSKU:-Out of stock
AZD 1152 is an orally bioavailable prodrug of AZD 1152-HQPA, a selective inhibitor of Aurora kinase B (IC50 = 0.36 nM).{31459} AZD 1152 is converted to AZD 1152-HQPA in plasma. Inhibition of Aurora B results in disruption of spindle checkpoint functions and chromosome alignment, resulting in inhibition of cytokinesis followed by apoptosis.{24932,19817} AZD 1152 inhibits tumor xenograft growth in vivo.{31460,31461}
Brand:CaymanSKU:- AZD 1152 is an orally bioavailable prodrug of AZD 1152-HQPA, a selective inhibitor of Aurora kinase B (IC50 = 0.36 nM).{31459} AZD 1152 is converted to AZD 1152-HQPA in plasma. Inhibition of Aurora B results in disruption of spindle checkpoint functions and chromosome alignment, resulting in inhibition of cytokinesis followed by apoptosis.{24932,19817} AZD 1152 inhibits tumor xenograft growth in vivo.{31460,31461}
Brand:CaymanSKU:- AZD 1152 is an orally bioavailable prodrug of AZD 1152-HQPA, a selective inhibitor of Aurora kinase B (IC50 = 0.36 nM).{31459} AZD 1152 is converted to AZD 1152-HQPA in plasma. Inhibition of Aurora B results in disruption of spindle checkpoint functions and chromosome alignment, resulting in inhibition of cytokinesis followed by apoptosis.{24932,19817} AZD 1152 inhibits tumor xenograft growth in vivo.{31460,31461}
Brand:CaymanSKU:- AZD 1152 is an orally bioavailable prodrug of AZD 1152-HQPA, a selective inhibitor of Aurora kinase B (IC50 = 0.36 nM).{31459} AZD 1152 is converted to AZD 1152-HQPA in plasma. Inhibition of Aurora B results in disruption of spindle checkpoint functions and chromosome alignment, resulting in inhibition of cytokinesis followed by apoptosis.{24932,19817} AZD 1152 inhibits tumor xenograft growth in vivo.{31460,31461}
Brand:CaymanSKU:-
AZD 1152-HQPA is an inhibitor of Aurora kinase B (IC50 = 0.37 nM) that demonstrates ~3,700-fold greater selectivity for Aurora kinase B over Aurora kinase A (IC50 = 1.368 µM).{31459,31461} It does not have activity against a panel of 50 other serine-threonine or tyrosine kinases, including FLT3, JAK2, and Abl.{31459,31461} AZD 1152-HQPA has been shown to inhibit the proliferation of hematopoietic malignant cells (IC50s = 3-40 nM), disrupting spindle checkpoint functions and chromosome alignment, resulting in inhibition of cytokinesis followed by apoptosis, and to inhibit tumor xenograft growth in vivo.{31461,31460}
Brand:CaymanSKU:11602 - 1 mgAvailable on backorder
AZD 1152-HQPA is an inhibitor of Aurora kinase B (IC50 = 0.37 nM) that demonstrates ~3,700-fold greater selectivity for Aurora kinase B over Aurora kinase A (IC50 = 1.368 µM).{31459,31461} It does not have activity against a panel of 50 other serine-threonine or tyrosine kinases, including FLT3, JAK2, and Abl.{31459,31461} AZD 1152-HQPA has been shown to inhibit the proliferation of hematopoietic malignant cells (IC50s = 3-40 nM), disrupting spindle checkpoint functions and chromosome alignment, resulting in inhibition of cytokinesis followed by apoptosis, and to inhibit tumor xenograft growth in vivo.{31461,31460}
Brand:CaymanSKU:11602 - 10 mgAvailable on backorder
AZD 1152-HQPA is an inhibitor of Aurora kinase B (IC50 = 0.37 nM) that demonstrates ~3,700-fold greater selectivity for Aurora kinase B over Aurora kinase A (IC50 = 1.368 µM).{31459,31461} It does not have activity against a panel of 50 other serine-threonine or tyrosine kinases, including FLT3, JAK2, and Abl.{31459,31461} AZD 1152-HQPA has been shown to inhibit the proliferation of hematopoietic malignant cells (IC50s = 3-40 nM), disrupting spindle checkpoint functions and chromosome alignment, resulting in inhibition of cytokinesis followed by apoptosis, and to inhibit tumor xenograft growth in vivo.{31461,31460}
Brand:CaymanSKU:11602 - 25 mgAvailable on backorder
AZD 1152-HQPA is an inhibitor of Aurora kinase B (IC50 = 0.37 nM) that demonstrates ~3,700-fold greater selectivity for Aurora kinase B over Aurora kinase A (IC50 = 1.368 µM).{31459,31461} It does not have activity against a panel of 50 other serine-threonine or tyrosine kinases, including FLT3, JAK2, and Abl.{31459,31461} AZD 1152-HQPA has been shown to inhibit the proliferation of hematopoietic malignant cells (IC50s = 3-40 nM), disrupting spindle checkpoint functions and chromosome alignment, resulting in inhibition of cytokinesis followed by apoptosis, and to inhibit tumor xenograft growth in vivo.{31461,31460}
Brand:CaymanSKU:11602 - 5 mgAvailable on backorder
AZD 1208 is a potent, selective, and orally available inhibitor of all three forms of the proto-oncogene Pim kinase (IC50s = 0.4, 5.0, and 1.9 nM for Pim-1, Pim-2, and Pim-3, respectively).{32021} It causes cell cycle arrest and apoptosis in MOLM-16 megakaryoblastic leukemia cells and inhibits the growth of MOLM-16 xenograft tumors in mice.{32021} It has efficacy against acute myeloid leukemia and glioblastoma cells when combined with mTOR and p110α inhibitors, respectively.{32019,32020}
Brand:CaymanSKU:20235 -Available on backorder
AZD 1208 is a potent, selective, and orally available inhibitor of all three forms of the proto-oncogene Pim kinase (IC50s = 0.4, 5.0, and 1.9 nM for Pim-1, Pim-2, and Pim-3, respectively).{32021} It causes cell cycle arrest and apoptosis in MOLM-16 megakaryoblastic leukemia cells and inhibits the growth of MOLM-16 xenograft tumors in mice.{32021} It has efficacy against acute myeloid leukemia and glioblastoma cells when combined with mTOR and p110α inhibitors, respectively.{32019,32020}
Brand:CaymanSKU:20235 -Available on backorder
AZD 1208 is a potent, selective, and orally available inhibitor of all three forms of the proto-oncogene Pim kinase (IC50s = 0.4, 5.0, and 1.9 nM for Pim-1, Pim-2, and Pim-3, respectively).{32021} It causes cell cycle arrest and apoptosis in MOLM-16 megakaryoblastic leukemia cells and inhibits the growth of MOLM-16 xenograft tumors in mice.{32021} It has efficacy against acute myeloid leukemia and glioblastoma cells when combined with mTOR and p110α inhibitors, respectively.{32019,32020}
Brand:CaymanSKU:20235 -Available on backorder
AZD 1208 is a potent, selective, and orally available inhibitor of all three forms of the proto-oncogene Pim kinase (IC50s = 0.4, 5.0, and 1.9 nM for Pim-1, Pim-2, and Pim-3, respectively).{32021} It causes cell cycle arrest and apoptosis in MOLM-16 megakaryoblastic leukemia cells and inhibits the growth of MOLM-16 xenograft tumors in mice.{32021} It has efficacy against acute myeloid leukemia and glioblastoma cells when combined with mTOR and p110α inhibitors, respectively.{32019,32020}
Brand:CaymanSKU:20235 -Available on backorder
AZD 1283 is an antagonist of the purinergic P2Y12 receptor (IC50 = 25 nM in a GTPγS assay in CHO cells).{52053} It selectively binds to the P2Y12 receptor (Kd = 11 nM) over more than 100 enzymes, receptors, and ion channels, including the P2Y1, platelet activating factor (PAF), and thromboxane A2 receptors, at 10 µM.{52053},{52054} AZD 1283 increases blood flow and inhibits platelet aggregation induced by ADP in a modified Folts dog model of thrombosis with ED50 values of 3 and 10 µg/kg per minute, respectively.
Brand:CaymanSKU:27649 - 1 mgAvailable on backorder
AZD 1283 is an antagonist of the purinergic P2Y12 receptor (IC50 = 25 nM in a GTPγS assay in CHO cells).{52053} It selectively binds to the P2Y12 receptor (Kd = 11 nM) over more than 100 enzymes, receptors, and ion channels, including the P2Y1, platelet activating factor (PAF), and thromboxane A2 receptors, at 10 µM.{52053},{52054} AZD 1283 increases blood flow and inhibits platelet aggregation induced by ADP in a modified Folts dog model of thrombosis with ED50 values of 3 and 10 µg/kg per minute, respectively.
Brand:CaymanSKU:27649 - 10 mgAvailable on backorder
AZD 1283 is an antagonist of the purinergic P2Y12 receptor (IC50 = 25 nM in a GTPγS assay in CHO cells).{52053} It selectively binds to the P2Y12 receptor (Kd = 11 nM) over more than 100 enzymes, receptors, and ion channels, including the P2Y1, platelet activating factor (PAF), and thromboxane A2 receptors, at 10 µM.{52053},{52054} AZD 1283 increases blood flow and inhibits platelet aggregation induced by ADP in a modified Folts dog model of thrombosis with ED50 values of 3 and 10 µg/kg per minute, respectively.
Brand:CaymanSKU:27649 - 25 mgAvailable on backorder
AZD 1283 is an antagonist of the purinergic P2Y12 receptor (IC50 = 25 nM in a GTPγS assay in CHO cells).{52053} It selectively binds to the P2Y12 receptor (Kd = 11 nM) over more than 100 enzymes, receptors, and ion channels, including the P2Y1, platelet activating factor (PAF), and thromboxane A2 receptors, at 10 µM.{52053},{52054} AZD 1283 increases blood flow and inhibits platelet aggregation induced by ADP in a modified Folts dog model of thrombosis with ED50 values of 3 and 10 µg/kg per minute, respectively.
Brand:CaymanSKU:27649 - 5 mgAvailable on backorder
AZD 1981 is a prostaglandin D2 (PGD2; Item No. 12010) receptor antagonist with a pIC50 value of 8.4 for CRTH2/DP2 and >1,000-fold selectivity over DP1.{32940} It has been shown to block functional responses in eosinophils, Th2 cells, and basophils and is currently under clinical evaluation as a potential therapeutic agent in respiratory diseases including asthma.{32940,32112}
Brand:CaymanSKU:20763 -Available on backorder
AZD 1981 is a prostaglandin D2 (PGD2; Item No. 12010) receptor antagonist with a pIC50 value of 8.4 for CRTH2/DP2 and >1,000-fold selectivity over DP1.{32940} It has been shown to block functional responses in eosinophils, Th2 cells, and basophils and is currently under clinical evaluation as a potential therapeutic agent in respiratory diseases including asthma.{32940,32112}
Brand:CaymanSKU:20763 -Available on backorder
AZD 1981 is a prostaglandin D2 (PGD2; Item No. 12010) receptor antagonist with a pIC50 value of 8.4 for CRTH2/DP2 and >1,000-fold selectivity over DP1.{32940} It has been shown to block functional responses in eosinophils, Th2 cells, and basophils and is currently under clinical evaluation as a potential therapeutic agent in respiratory diseases including asthma.{32940,32112}
Brand:CaymanSKU:20763 -Available on backorder
AZD 1981 is a prostaglandin D2 (PGD2; Item No. 12010) receptor antagonist with a pIC50 value of 8.4 for CRTH2/DP2 and >1,000-fold selectivity over DP1.{32940} It has been shown to block functional responses in eosinophils, Th2 cells, and basophils and is currently under clinical evaluation as a potential therapeutic agent in respiratory diseases including asthma.{32940,32112}
Brand:CaymanSKU:20763 -Available on backorder
AZD 2014 is a potent, selective, ATP-competitive mTORC1/2 dual inhibitor that inhibits phosphorylation of both mTORC1 and 2 substrate proteins in whole cells.{33186} It exhibits an IC50 value of 2.81 nM against the isolated recombinant enzyme and >1,000-fold selectivity against all PI3K isoforms.{33186} AZD 2014 has broad antiproliferative effects across multiple cell lines and reduces tumor growth in in vivo models of ER+ breast cancer.{33186}. It has efficacy against acute myeloid leukemia when combined with the pan Pim kinase inhibitor AZD 1208 (Item No. 20235) and enhances the radiosensitivity of different cancer cell types.{32019,33187,33188}
Brand:CaymanSKU:-Available on backorder
AZD 2014 is a potent, selective, ATP-competitive mTORC1/2 dual inhibitor that inhibits phosphorylation of both mTORC1 and 2 substrate proteins in whole cells.{33186} It exhibits an IC50 value of 2.81 nM against the isolated recombinant enzyme and >1,000-fold selectivity against all PI3K isoforms.{33186} AZD 2014 has broad antiproliferative effects across multiple cell lines and reduces tumor growth in in vivo models of ER+ breast cancer.{33186}. It has efficacy against acute myeloid leukemia when combined with the pan Pim kinase inhibitor AZD 1208 (Item No. 20235) and enhances the radiosensitivity of different cancer cell types.{32019,33187,33188}
Brand:CaymanSKU:-Available on backorder
AZD 2014 is a potent, selective, ATP-competitive mTORC1/2 dual inhibitor that inhibits phosphorylation of both mTORC1 and 2 substrate proteins in whole cells.{33186} It exhibits an IC50 value of 2.81 nM against the isolated recombinant enzyme and >1,000-fold selectivity against all PI3K isoforms.{33186} AZD 2014 has broad antiproliferative effects across multiple cell lines and reduces tumor growth in in vivo models of ER+ breast cancer.{33186}. It has efficacy against acute myeloid leukemia when combined with the pan Pim kinase inhibitor AZD 1208 (Item No. 20235) and enhances the radiosensitivity of different cancer cell types.{32019,33187,33188}
Brand:CaymanSKU:-Available on backorder
AZD 2014 is a potent, selective, ATP-competitive mTORC1/2 dual inhibitor that inhibits phosphorylation of both mTORC1 and 2 substrate proteins in whole cells.{33186} It exhibits an IC50 value of 2.81 nM against the isolated recombinant enzyme and >1,000-fold selectivity against all PI3K isoforms.{33186} AZD 2014 has broad antiproliferative effects across multiple cell lines and reduces tumor growth in in vivo models of ER+ breast cancer.{33186}. It has efficacy against acute myeloid leukemia when combined with the pan Pim kinase inhibitor AZD 1208 (Item No. 20235) and enhances the radiosensitivity of different cancer cell types.{32019,33187,33188}
Brand:CaymanSKU:-Available on backorder
AZD 2098 is a CC chemokine receptor 4 (CCR4) antagonist.{50101} AZD 2098 inhibits CCL22-induced calcium flux in CHO cells expressing human recombinant CCR4 (IC50 = 31.6 nM) and CCL22- and CCL17-mediated Th2 cell chemotaxis (IC50 = 501.2 nM for both). AZD 2098 is selective for CCR4 over CXCR1, CXCR2, CCR1, CCR2b, CCR5, CCR7, and CCR8 up to 10 µM in vitro. Administration of AZD 2098 (0.07-2.5 mg/kg, p.o.) to ovalbumin-sensitized, antigen-challenged rats reduces alveolitis and leukocyte infiltration in the lung in a dose-dependent manner.
Brand:CaymanSKU:27633 - 1 mgAvailable on backorder
AZD 2098 is a CC chemokine receptor 4 (CCR4) antagonist.{50101} AZD 2098 inhibits CCL22-induced calcium flux in CHO cells expressing human recombinant CCR4 (IC50 = 31.6 nM) and CCL22- and CCL17-mediated Th2 cell chemotaxis (IC50 = 501.2 nM for both). AZD 2098 is selective for CCR4 over CXCR1, CXCR2, CCR1, CCR2b, CCR5, CCR7, and CCR8 up to 10 µM in vitro. Administration of AZD 2098 (0.07-2.5 mg/kg, p.o.) to ovalbumin-sensitized, antigen-challenged rats reduces alveolitis and leukocyte infiltration in the lung in a dose-dependent manner.
Brand:CaymanSKU:27633 - 10 mgAvailable on backorder
AZD 2098 is a CC chemokine receptor 4 (CCR4) antagonist.{50101} AZD 2098 inhibits CCL22-induced calcium flux in CHO cells expressing human recombinant CCR4 (IC50 = 31.6 nM) and CCL22- and CCL17-mediated Th2 cell chemotaxis (IC50 = 501.2 nM for both). AZD 2098 is selective for CCR4 over CXCR1, CXCR2, CCR1, CCR2b, CCR5, CCR7, and CCR8 up to 10 µM in vitro. Administration of AZD 2098 (0.07-2.5 mg/kg, p.o.) to ovalbumin-sensitized, antigen-challenged rats reduces alveolitis and leukocyte infiltration in the lung in a dose-dependent manner.
Brand:CaymanSKU:27633 - 25 mgAvailable on backorder
AZD 2098 is a CC chemokine receptor 4 (CCR4) antagonist.{50101} AZD 2098 inhibits CCL22-induced calcium flux in CHO cells expressing human recombinant CCR4 (IC50 = 31.6 nM) and CCL22- and CCL17-mediated Th2 cell chemotaxis (IC50 = 501.2 nM for both). AZD 2098 is selective for CCR4 over CXCR1, CXCR2, CCR1, CCR2b, CCR5, CCR7, and CCR8 up to 10 µM in vitro. Administration of AZD 2098 (0.07-2.5 mg/kg, p.o.) to ovalbumin-sensitized, antigen-challenged rats reduces alveolitis and leukocyte infiltration in the lung in a dose-dependent manner.
Brand:CaymanSKU:27633 - 5 mgAvailable on backorder
The poly(ADP-ribose) polymerases (PARPs) form a family of enzymes with roles in DNA repair and apoptosis, particularly in response to reactive oxygen and nitrogen species. AZD 2461 is a PARP inhibitor (IC50 = 5 nM) with low affinity for the P-glycoprotein drug efflux transporter.{31078} It was developed to overcome the resistance encountered with olaparib (Item No. 10621) that is presumed to be mediated in part by P-glycoprotein-mediated drug efflux.{31078} When tested on the olaparib-resistant KB1P tumor T6-28, which has an 80-fold increased Mdr1b expression, AZD 2461 did not affect P-glycoprotein.{31078} Furthermore, it can induce a loss of p53 binding protein 1 expression in mice with KB1P tumors at 100 mg/kg.{31078}
Brand:CaymanSKU:-Out of stock
The poly(ADP-ribose) polymerases (PARPs) form a family of enzymes with roles in DNA repair and apoptosis, particularly in response to reactive oxygen and nitrogen species. AZD 2461 is a PARP inhibitor (IC50 = 5 nM) with low affinity for the P-glycoprotein drug efflux transporter.{31078} It was developed to overcome the resistance encountered with olaparib (Item No. 10621) that is presumed to be mediated in part by P-glycoprotein-mediated drug efflux.{31078} When tested on the olaparib-resistant KB1P tumor T6-28, which has an 80-fold increased Mdr1b expression, AZD 2461 did not affect P-glycoprotein.{31078} Furthermore, it can induce a loss of p53 binding protein 1 expression in mice with KB1P tumors at 100 mg/kg.{31078}
Brand:CaymanSKU:-Out of stock
The poly(ADP-ribose) polymerases (PARPs) form a family of enzymes with roles in DNA repair and apoptosis, particularly in response to reactive oxygen and nitrogen species. AZD 2461 is a PARP inhibitor (IC50 = 5 nM) with low affinity for the P-glycoprotein drug efflux transporter.{31078} It was developed to overcome the resistance encountered with olaparib (Item No. 10621) that is presumed to be mediated in part by P-glycoprotein-mediated drug efflux.{31078} When tested on the olaparib-resistant KB1P tumor T6-28, which has an 80-fold increased Mdr1b expression, AZD 2461 did not affect P-glycoprotein.{31078} Furthermore, it can induce a loss of p53 binding protein 1 expression in mice with KB1P tumors at 100 mg/kg.{31078}
Brand:CaymanSKU:-Out of stock
The poly(ADP-ribose) polymerases (PARPs) form a family of enzymes with roles in DNA repair and apoptosis, particularly in response to reactive oxygen and nitrogen species. AZD 2461 is a PARP inhibitor (IC50 = 5 nM) with low affinity for the P-glycoprotein drug efflux transporter.{31078} It was developed to overcome the resistance encountered with olaparib (Item No. 10621) that is presumed to be mediated in part by P-glycoprotein-mediated drug efflux.{31078} When tested on the olaparib-resistant KB1P tumor T6-28, which has an 80-fold increased Mdr1b expression, AZD 2461 did not affect P-glycoprotein.{31078} Furthermore, it can induce a loss of p53 binding protein 1 expression in mice with KB1P tumors at 100 mg/kg.{31078}
Brand:CaymanSKU:-Out of stock
Glycogen synthase kinase 3β (GSK3β) was originally identified for its ability to constitutively phosphorylate and inactivate glycogen synthase, preventing glycogen synthesis.{19045} It can also phosphorylate proteins that are relevant to osteogenesis and Alzheimer’s disease, the latter for which it has earned the moniker, tau phosphorylating kinase.{25567,25565,25566} AZD 2858 is a pyrazine analog that inhibits GSK3β with a Ki value of 4.9 nM.{27205} It crosses the blood brain barrier and inhibits tau phosphorylation in vitro with an IC50 value of 76 nM.{27205} AZD 2858 has also been shown to increase bone mass (via Wnt activation) in rats after a two-week treatment with a maximum effective oral dose of 20 mg/kg once daily.{27203} Furthermore, by inhibiting GSK3β, AZD 2858 can stabilize β-catenin in rat mesenchymal stem cells (EC50 = 234 nM), spurring osteoblast differentiation.{27204}
Brand:CaymanSKU:-Out of stock
Glycogen synthase kinase 3β (GSK3β) was originally identified for its ability to constitutively phosphorylate and inactivate glycogen synthase, preventing glycogen synthesis.{19045} It can also phosphorylate proteins that are relevant to osteogenesis and Alzheimer’s disease, the latter for which it has earned the moniker, tau phosphorylating kinase.{25567,25565,25566} AZD 2858 is a pyrazine analog that inhibits GSK3β with a Ki value of 4.9 nM.{27205} It crosses the blood brain barrier and inhibits tau phosphorylation in vitro with an IC50 value of 76 nM.{27205} AZD 2858 has also been shown to increase bone mass (via Wnt activation) in rats after a two-week treatment with a maximum effective oral dose of 20 mg/kg once daily.{27203} Furthermore, by inhibiting GSK3β, AZD 2858 can stabilize β-catenin in rat mesenchymal stem cells (EC50 = 234 nM), spurring osteoblast differentiation.{27204}
Brand:CaymanSKU:-Out of stock
Glycogen synthase kinase 3β (GSK3β) was originally identified for its ability to constitutively phosphorylate and inactivate glycogen synthase, preventing glycogen synthesis.{19045} It can also phosphorylate proteins that are relevant to osteogenesis and Alzheimer’s disease, the latter for which it has earned the moniker, tau phosphorylating kinase.{25567,25565,25566} AZD 2858 is a pyrazine analog that inhibits GSK3β with a Ki value of 4.9 nM.{27205} It crosses the blood brain barrier and inhibits tau phosphorylation in vitro with an IC50 value of 76 nM.{27205} AZD 2858 has also been shown to increase bone mass (via Wnt activation) in rats after a two-week treatment with a maximum effective oral dose of 20 mg/kg once daily.{27203} Furthermore, by inhibiting GSK3β, AZD 2858 can stabilize β-catenin in rat mesenchymal stem cells (EC50 = 234 nM), spurring osteoblast differentiation.{27204}
Brand:CaymanSKU:-Out of stock
AZD 2932 is an inhibitor of VEGFR2, PDGFRβ, CSF1R, c-KIT, and FLT3 receptor tyrosine kinases (IC50s = 4, 8, 100, 9, and 7 nM, respectively).{41214} It also inhibits Pdgfrα phosphorylation (IC50 = 2 nM) in lysates from C6 rat glial tumors grown in athymic mice. AZD 2932 (12.5-50 mg/kg) reduces tumor growth and inhibits Pdgfrβ and Vegfr2 phosphorylation in a 1:1 ratio in a C6 mouse xenograft model. Xenograft models using non-PDGFR expressing tumor cells were insensitive to AZD 2932 treatment.
Brand:CaymanSKU:-Available on backorder
AZD 2932 is an inhibitor of VEGFR2, PDGFRβ, CSF1R, c-KIT, and FLT3 receptor tyrosine kinases (IC50s = 4, 8, 100, 9, and 7 nM, respectively).{41214} It also inhibits Pdgfrα phosphorylation (IC50 = 2 nM) in lysates from C6 rat glial tumors grown in athymic mice. AZD 2932 (12.5-50 mg/kg) reduces tumor growth and inhibits Pdgfrβ and Vegfr2 phosphorylation in a 1:1 ratio in a C6 mouse xenograft model. Xenograft models using non-PDGFR expressing tumor cells were insensitive to AZD 2932 treatment.
Brand:CaymanSKU:-Available on backorder
AZD 2932 is an inhibitor of VEGFR2, PDGFRβ, CSF1R, c-KIT, and FLT3 receptor tyrosine kinases (IC50s = 4, 8, 100, 9, and 7 nM, respectively).{41214} It also inhibits Pdgfrα phosphorylation (IC50 = 2 nM) in lysates from C6 rat glial tumors grown in athymic mice. AZD 2932 (12.5-50 mg/kg) reduces tumor growth and inhibits Pdgfrβ and Vegfr2 phosphorylation in a 1:1 ratio in a C6 mouse xenograft model. Xenograft models using non-PDGFR expressing tumor cells were insensitive to AZD 2932 treatment.
Brand:CaymanSKU:-Available on backorder
AZD 2932 is an inhibitor of VEGFR2, PDGFRβ, CSF1R, c-KIT, and FLT3 receptor tyrosine kinases (IC50s = 4, 8, 100, 9, and 7 nM, respectively).{41214} It also inhibits Pdgfrα phosphorylation (IC50 = 2 nM) in lysates from C6 rat glial tumors grown in athymic mice. AZD 2932 (12.5-50 mg/kg) reduces tumor growth and inhibits Pdgfrβ and Vegfr2 phosphorylation in a 1:1 ratio in a C6 mouse xenograft model. Xenograft models using non-PDGFR expressing tumor cells were insensitive to AZD 2932 treatment.
Brand:CaymanSKU:-Available on backorder
AZD 3147 is an orally bioavailable dual inhibitor of mammalian target of rapamycin complex 1 (mTORC1) and mTORC2 (IC50s = 40.7 and 5.75 nM, respectively, in MDA-MB-468 cells).{55175} It is selective for mTOR over PI3Kα, PI3Kβ, PI3Kδ, and PI3Kγ (IC50s = 1.51, 912, 5,495, 9,333, and 6,310 nM, respectively, in enzyme assays).
Brand:CaymanSKU:22474 -Out of stock
AZD 3147 is an orally bioavailable dual inhibitor of mammalian target of rapamycin complex 1 (mTORC1) and mTORC2 (IC50s = 40.7 and 5.75 nM, respectively, in MDA-MB-468 cells).{55175} It is selective for mTOR over PI3Kα, PI3Kβ, PI3Kδ, and PI3Kγ (IC50s = 1.51, 912, 5,495, 9,333, and 6,310 nM, respectively, in enzyme assays).
Brand:CaymanSKU:22474 -Out of stock
AZD 3147 is an orally bioavailable dual inhibitor of mammalian target of rapamycin complex 1 (mTORC1) and mTORC2 (IC50s = 40.7 and 5.75 nM, respectively, in MDA-MB-468 cells).{55175} It is selective for mTOR over PI3Kα, PI3Kβ, PI3Kδ, and PI3Kγ (IC50s = 1.51, 912, 5,495, 9,333, and 6,310 nM, respectively, in enzyme assays).
Brand:CaymanSKU:22474 -Out of stock
AZD 3147 is an orally bioavailable dual inhibitor of mammalian target of rapamycin complex 1 (mTORC1) and mTORC2 (IC50s = 40.7 and 5.75 nM, respectively, in MDA-MB-468 cells).{55175} It is selective for mTOR over PI3Kα, PI3Kβ, PI3Kδ, and PI3Kγ (IC50s = 1.51, 912, 5,495, 9,333, and 6,310 nM, respectively, in enzyme assays).
Brand:CaymanSKU:22474 -Out of stock
AZD 3229 is an inhibitor of c-Kit-driven cell proliferation.{51097} It selectively inhibits growth of c-Kit mutant (GI50s = 1-971 nM) and PDGFR mutant (GI50s = 1-22 nM) Ba/F3 cell lines over Ba/F3 cell lines expressing Tel-KDR/VEGFR2 (GI50 = 1,378 nM). AZD 3229 (20 mg/kg twice per day) induces tumor regression in a Ba/F3 mouse xenograft model and a mouse allograft model using Ba/F3 cells expressing KIT-exon 11 del/V654A, a common mutation in gastrointestinal stromal tumors (GIST).
Brand:CaymanSKU:27908 - 1 mgAvailable on backorder
AZD 3229 is an inhibitor of c-Kit-driven cell proliferation.{51097} It selectively inhibits growth of c-Kit mutant (GI50s = 1-971 nM) and PDGFR mutant (GI50s = 1-22 nM) Ba/F3 cell lines over Ba/F3 cell lines expressing Tel-KDR/VEGFR2 (GI50 = 1,378 nM). AZD 3229 (20 mg/kg twice per day) induces tumor regression in a Ba/F3 mouse xenograft model and a mouse allograft model using Ba/F3 cells expressing KIT-exon 11 del/V654A, a common mutation in gastrointestinal stromal tumors (GIST).
Brand:CaymanSKU:27908 - 5 mgAvailable on backorder
AZD 3229 is an inhibitor of c-Kit-driven cell proliferation.{51097} It selectively inhibits growth of c-Kit mutant (GI50s = 1-971 nM) and PDGFR mutant (GI50s = 1-22 nM) Ba/F3 cell lines over Ba/F3 cell lines expressing Tel-KDR/VEGFR2 (GI50 = 1,378 nM). AZD 3229 (20 mg/kg twice per day) induces tumor regression in a Ba/F3 mouse xenograft model and a mouse allograft model using Ba/F3 cells expressing KIT-exon 11 del/V654A, a common mutation in gastrointestinal stromal tumors (GIST).
Brand:CaymanSKU:27908 - 500 µgAvailable on backorder
Brand:CaymanSKU:-Available on backorder
Brand:CaymanSKU:-Available on backorder
Brand:CaymanSKU:-Available on backorder
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AZD 3463 is an inhibitor of anaplastic lymphoma kinase (ALK) and the insulin growth factor-1 receptor (IGF-1R).{43620} It inhibits ALK with an IC50 value of 15 nM.{38680} It inhibits the proliferation of neuroblastoma cells with wild-type (WT) ALK (IC50s = 2.8-21.3 µM) and ALK with the activating mutations ALKF1174L and ALKD1091N (IC50s = 1.7 and 16.49 µM, respectively) and induces apoptosis and autophagy.{43620} It reduces tumor growth in neuroblastoma mouse xenograft models expressing WT ALK or the ALKF1174L mutation when administered at a dose of 15 mg/kg per day for 21 days.
Brand:CaymanSKU:26172 - 1 mgAvailable on backorder
AZD 3463 is an inhibitor of anaplastic lymphoma kinase (ALK) and the insulin growth factor-1 receptor (IGF-1R).{43620} It inhibits ALK with an IC50 value of 15 nM.{38680} It inhibits the proliferation of neuroblastoma cells with wild-type (WT) ALK (IC50s = 2.8-21.3 µM) and ALK with the activating mutations ALKF1174L and ALKD1091N (IC50s = 1.7 and 16.49 µM, respectively) and induces apoptosis and autophagy.{43620} It reduces tumor growth in neuroblastoma mouse xenograft models expressing WT ALK or the ALKF1174L mutation when administered at a dose of 15 mg/kg per day for 21 days.
Brand:CaymanSKU:26172 - 10 mgAvailable on backorder
AZD 3463 is an inhibitor of anaplastic lymphoma kinase (ALK) and the insulin growth factor-1 receptor (IGF-1R).{43620} It inhibits ALK with an IC50 value of 15 nM.{38680} It inhibits the proliferation of neuroblastoma cells with wild-type (WT) ALK (IC50s = 2.8-21.3 µM) and ALK with the activating mutations ALKF1174L and ALKD1091N (IC50s = 1.7 and 16.49 µM, respectively) and induces apoptosis and autophagy.{43620} It reduces tumor growth in neuroblastoma mouse xenograft models expressing WT ALK or the ALKF1174L mutation when administered at a dose of 15 mg/kg per day for 21 days.
Brand:CaymanSKU:26172 - 25 mgAvailable on backorder
AZD 3463 is an inhibitor of anaplastic lymphoma kinase (ALK) and the insulin growth factor-1 receptor (IGF-1R).{43620} It inhibits ALK with an IC50 value of 15 nM.{38680} It inhibits the proliferation of neuroblastoma cells with wild-type (WT) ALK (IC50s = 2.8-21.3 µM) and ALK with the activating mutations ALKF1174L and ALKD1091N (IC50s = 1.7 and 16.49 µM, respectively) and induces apoptosis and autophagy.{43620} It reduces tumor growth in neuroblastoma mouse xenograft models expressing WT ALK or the ALKF1174L mutation when administered at a dose of 15 mg/kg per day for 21 days.
Brand:CaymanSKU:26172 - 5 mgAvailable on backorder
AZD 3759 is a brain penetrant inhibitor of wild-type and constitutively active mutant EGF receptors (EGFRs; IC50s = 0.3, 0.2, and 0.2 nM for wild-type, L858R-mutant, and exon 19 deletion-containing EGFRs, respectively).{41251} It is selective for EGFR over 115 other kinases, exhibiting 50s = 7.7 and 7.0 nM, respectively) but has no effect on H838 cells that express wild-type EGFR (GI50 = 21,556 nM). AZD 3759 inhibits tumor growth by 78% and induces tumor regression at doses of 7.5 and 15 mg/kg, p.o., respectively in a PC-9 mouse model of non-small cell lung cancer (NSCLC) brain metastasis.
Brand:CaymanSKU:19931 -Available on backorder
AZD 3759 is a brain penetrant inhibitor of wild-type and constitutively active mutant EGF receptors (EGFRs; IC50s = 0.3, 0.2, and 0.2 nM for wild-type, L858R-mutant, and exon 19 deletion-containing EGFRs, respectively).{41251} It is selective for EGFR over 115 other kinases, exhibiting 50s = 7.7 and 7.0 nM, respectively) but has no effect on H838 cells that express wild-type EGFR (GI50 = 21,556 nM). AZD 3759 inhibits tumor growth by 78% and induces tumor regression at doses of 7.5 and 15 mg/kg, p.o., respectively in a PC-9 mouse model of non-small cell lung cancer (NSCLC) brain metastasis.
Brand:CaymanSKU:19931 -Available on backorder
AZD 3759 is a brain penetrant inhibitor of wild-type and constitutively active mutant EGF receptors (EGFRs; IC50s = 0.3, 0.2, and 0.2 nM for wild-type, L858R-mutant, and exon 19 deletion-containing EGFRs, respectively).{41251} It is selective for EGFR over 115 other kinases, exhibiting 50s = 7.7 and 7.0 nM, respectively) but has no effect on H838 cells that express wild-type EGFR (GI50 = 21,556 nM). AZD 3759 inhibits tumor growth by 78% and induces tumor regression at doses of 7.5 and 15 mg/kg, p.o., respectively in a PC-9 mouse model of non-small cell lung cancer (NSCLC) brain metastasis.
Brand:CaymanSKU:19931 -Available on backorder
AZD 3759 is a brain penetrant inhibitor of wild-type and constitutively active mutant EGF receptors (EGFRs; IC50s = 0.3, 0.2, and 0.2 nM for wild-type, L858R-mutant, and exon 19 deletion-containing EGFRs, respectively).{41251} It is selective for EGFR over 115 other kinases, exhibiting 50s = 7.7 and 7.0 nM, respectively) but has no effect on H838 cells that express wild-type EGFR (GI50 = 21,556 nM). AZD 3759 inhibits tumor growth by 78% and induces tumor regression at doses of 7.5 and 15 mg/kg, p.o., respectively in a PC-9 mouse model of non-small cell lung cancer (NSCLC) brain metastasis.
Brand:CaymanSKU:19931 -Available on backorder
AZD 3965 is a potent inhibitor of monocarboxylate transporter 1 (MCT1; Ki = 1.6 nM), killing tumor cells that are reliant on glycolysis by blocking lactate transport.{32004} It displays six-fold selectivity for MCT1 over MCT2 and is without effect against MCT4 at 10 µM. AZD 3965 increases intratumor lactate levels and decreases tumor growth in mice bearing COR-L103 small cell lung cancer (SCLC) xenografts.{32004} AZD 3965 also enhances radiosensitivity in mice with SCLC xenografts.{32003}
Brand:CaymanSKU:19912 -Available on backorder
AZD 3965 is a potent inhibitor of monocarboxylate transporter 1 (MCT1; Ki = 1.6 nM), killing tumor cells that are reliant on glycolysis by blocking lactate transport.{32004} It displays six-fold selectivity for MCT1 over MCT2 and is without effect against MCT4 at 10 µM. AZD 3965 increases intratumor lactate levels and decreases tumor growth in mice bearing COR-L103 small cell lung cancer (SCLC) xenografts.{32004} AZD 3965 also enhances radiosensitivity in mice with SCLC xenografts.{32003}
Brand:CaymanSKU:19912 -Available on backorder
AZD 3965 is a potent inhibitor of monocarboxylate transporter 1 (MCT1; Ki = 1.6 nM), killing tumor cells that are reliant on glycolysis by blocking lactate transport.{32004} It displays six-fold selectivity for MCT1 over MCT2 and is without effect against MCT4 at 10 µM. AZD 3965 increases intratumor lactate levels and decreases tumor growth in mice bearing COR-L103 small cell lung cancer (SCLC) xenografts.{32004} AZD 3965 also enhances radiosensitivity in mice with SCLC xenografts.{32003}
Brand:CaymanSKU:19912 -Available on backorder
AZD 3965 is a potent inhibitor of monocarboxylate transporter 1 (MCT1; Ki = 1.6 nM), killing tumor cells that are reliant on glycolysis by blocking lactate transport.{32004} It displays six-fold selectivity for MCT1 over MCT2 and is without effect against MCT4 at 10 µM. AZD 3965 increases intratumor lactate levels and decreases tumor growth in mice bearing COR-L103 small cell lung cancer (SCLC) xenografts.{32004} AZD 3965 also enhances radiosensitivity in mice with SCLC xenografts.{32003}
Brand:CaymanSKU:19912 -Available on backorder
AZD 4547 is a selective inhibitor of the fibroblast growth factor receptor (FGFR) tyrosine kinase with IC50 values of 0.2, 2.5, and 1.8 nM for FGFR1, 2, and 3, respectively.{24741} It displays weaker activity against FGFR4 (IC50 = 165 nM), VEGFR2 (IC50 = 24 nM), and a panel of other tyrosine and serine/theronine kinases such as insulin-like growth factor 1 receptor (IC50 = 581 nM), cyclin-dependent kinase 2 (IC50 = >10 μM), and p38 (IC50 = >100 μM).{24741} AZD 4547 has demonstrated antiproliferative activity in tumor cell lines expressing deregulated FGFRs (IC50s = 18-281 nM).{24741} In an FGFR-driven human tumor xenograft mouse model, oral administration of AZD 4547 at concentrations up to 12.5 mg/kg/day resulted in potent dose-dependent antitumor activity.{24741}
Brand:CaymanSKU:- AZD 4547 is a selective inhibitor of the fibroblast growth factor receptor (FGFR) tyrosine kinase with IC50 values of 0.2, 2.5, and 1.8 nM for FGFR1, 2, and 3, respectively.{24741} It displays weaker activity against FGFR4 (IC50 = 165 nM), VEGFR2 (IC50 = 24 nM), and a panel of other tyrosine and serine/theronine kinases such as insulin-like growth factor 1 receptor (IC50 = 581 nM), cyclin-dependent kinase 2 (IC50 = >10 μM), and p38 (IC50 = >100 μM).{24741} AZD 4547 has demonstrated antiproliferative activity in tumor cell lines expressing deregulated FGFRs (IC50s = 18-281 nM).{24741} In an FGFR-driven human tumor xenograft mouse model, oral administration of AZD 4547 at concentrations up to 12.5 mg/kg/day resulted in potent dose-dependent antitumor activity.{24741}
Brand:CaymanSKU:- AZD 4547 is a selective inhibitor of the fibroblast growth factor receptor (FGFR) tyrosine kinase with IC50 values of 0.2, 2.5, and 1.8 nM for FGFR1, 2, and 3, respectively.{24741} It displays weaker activity against FGFR4 (IC50 = 165 nM), VEGFR2 (IC50 = 24 nM), and a panel of other tyrosine and serine/theronine kinases such as insulin-like growth factor 1 receptor (IC50 = 581 nM), cyclin-dependent kinase 2 (IC50 = >10 μM), and p38 (IC50 = >100 μM).{24741} AZD 4547 has demonstrated antiproliferative activity in tumor cell lines expressing deregulated FGFRs (IC50s = 18-281 nM).{24741} In an FGFR-driven human tumor xenograft mouse model, oral administration of AZD 4547 at concentrations up to 12.5 mg/kg/day resulted in potent dose-dependent antitumor activity.{24741}
Brand:CaymanSKU:-
AZD 4635 is an adenosine A2 receptor antagonist (Ki = 1.7 nM for the human receptor).{47334} It inhibits adenosine-induced cAMP production in CHO cells expressing the human A2 receptor (IC50 = 0.79 μM) and reverses suppression of IFN-γ secretion induced by 5′-N-ethylcarboxamidoadenosine (NECA; Item No. 21420) in CD8+ T cells. AZD 4635 reduces tumor growth when administered alone and in combination with checkpoint inhibitors in syngeneic mouse tumor models.
Brand:CaymanSKU:26322 - 10 mgAvailable on backorder
AZD 4635 is an adenosine A2 receptor antagonist (Ki = 1.7 nM for the human receptor).{47334} It inhibits adenosine-induced cAMP production in CHO cells expressing the human A2 receptor (IC50 = 0.79 μM) and reverses suppression of IFN-γ secretion induced by 5′-N-ethylcarboxamidoadenosine (NECA; Item No. 21420) in CD8+ T cells. AZD 4635 reduces tumor growth when administered alone and in combination with checkpoint inhibitors in syngeneic mouse tumor models.
Brand:CaymanSKU:26322 - 25 mgAvailable on backorder
AZD 4635 is an adenosine A2 receptor antagonist (Ki = 1.7 nM for the human receptor).{47334} It inhibits adenosine-induced cAMP production in CHO cells expressing the human A2 receptor (IC50 = 0.79 μM) and reverses suppression of IFN-γ secretion induced by 5′-N-ethylcarboxamidoadenosine (NECA; Item No. 21420) in CD8+ T cells. AZD 4635 reduces tumor growth when administered alone and in combination with checkpoint inhibitors in syngeneic mouse tumor models.
Brand:CaymanSKU:26322 - 5 mgAvailable on backorder
AZD 4635 is an adenosine A2 receptor antagonist (Ki = 1.7 nM for the human receptor).{47334} It inhibits adenosine-induced cAMP production in CHO cells expressing the human A2 receptor (IC50 = 0.79 μM) and reverses suppression of IFN-γ secretion induced by 5′-N-ethylcarboxamidoadenosine (NECA; Item No. 21420) in CD8+ T cells. AZD 4635 reduces tumor growth when administered alone and in combination with checkpoint inhibitors in syngeneic mouse tumor models.
Brand:CaymanSKU:26322 - 50 mgAvailable on backorder
AZD 5069 is an antagonist of chemokine receptor 2 (CXCR2; IC50 = 0.79 nM in a radioligand binding assay).{45374} It inhibits CXCL1-induced CD11b expression in and chemotaxis of isolated human neutrophils (pA2s = 6.9 and 9.1, respectively). AZD 5069 (3 and 10 μmol/kg) inhibits bronchoalveolar lavage fluid (BALF) neutrophil influx in a rat model of LPS-induced lung neutrophilia and non-allergic airway inflammation.
Brand:CaymanSKU:28297 - 1 mgAvailable on backorder
AZD 5069 is an antagonist of chemokine receptor 2 (CXCR2; IC50 = 0.79 nM in a radioligand binding assay).{45374} It inhibits CXCL1-induced CD11b expression in and chemotaxis of isolated human neutrophils (pA2s = 6.9 and 9.1, respectively). AZD 5069 (3 and 10 μmol/kg) inhibits bronchoalveolar lavage fluid (BALF) neutrophil influx in a rat model of LPS-induced lung neutrophilia and non-allergic airway inflammation.
Brand:CaymanSKU:28297 - 10 mgAvailable on backorder
AZD 5069 is an antagonist of chemokine receptor 2 (CXCR2; IC50 = 0.79 nM in a radioligand binding assay).{45374} It inhibits CXCL1-induced CD11b expression in and chemotaxis of isolated human neutrophils (pA2s = 6.9 and 9.1, respectively). AZD 5069 (3 and 10 μmol/kg) inhibits bronchoalveolar lavage fluid (BALF) neutrophil influx in a rat model of LPS-induced lung neutrophilia and non-allergic airway inflammation.
Brand:CaymanSKU:28297 - 25 mgAvailable on backorder
AZD 5069 is an antagonist of chemokine receptor 2 (CXCR2; IC50 = 0.79 nM in a radioligand binding assay).{45374} It inhibits CXCL1-induced CD11b expression in and chemotaxis of isolated human neutrophils (pA2s = 6.9 and 9.1, respectively). AZD 5069 (3 and 10 μmol/kg) inhibits bronchoalveolar lavage fluid (BALF) neutrophil influx in a rat model of LPS-induced lung neutrophilia and non-allergic airway inflammation.
Brand:CaymanSKU:28297 - 5 mgAvailable on backorder
AZD 5153 an orally available, bivalent inhibitor of the bromodomain and extraterminal (BET) protein BRD4 (IC50 = 5 nM).{32416} It can simultaneously bind two bromodomains in BRD4, which has been shown to increase antitumor activity in multiple xenograft models of acute myeloid leukemia, multiple myeloma, and diffuse large B cell lymphoma.{32416}
Brand:CaymanSKU:20864 -Out of stock
AZD 5153 an orally available, bivalent inhibitor of the bromodomain and extraterminal (BET) protein BRD4 (IC50 = 5 nM).{32416} It can simultaneously bind two bromodomains in BRD4, which has been shown to increase antitumor activity in multiple xenograft models of acute myeloid leukemia, multiple myeloma, and diffuse large B cell lymphoma.{32416}
Brand:CaymanSKU:20864 -Out of stock
AZD 5153 an orally available, bivalent inhibitor of the bromodomain and extraterminal (BET) protein BRD4 (IC50 = 5 nM).{32416} It can simultaneously bind two bromodomains in BRD4, which has been shown to increase antitumor activity in multiple xenograft models of acute myeloid leukemia, multiple myeloma, and diffuse large B cell lymphoma.{32416}
Brand:CaymanSKU:20864 -Out of stock
AZD 5153 an orally available, bivalent inhibitor of the bromodomain and extraterminal (BET) protein BRD4 (IC50 = 5 nM).{32416} It can simultaneously bind two bromodomains in BRD4, which has been shown to increase antitumor activity in multiple xenograft models of acute myeloid leukemia, multiple myeloma, and diffuse large B cell lymphoma.{32416}
Brand:CaymanSKU:20864 -Out of stock
Akt functions as a key component in multiple signaling pathways including those related to cell proliferation, metabolism, and survival as well as angiogenesis. AZD 5363 is a pyrrolopyrimidine-derived compound that inhibits Akt by competitively binding to the kinase domain, preventing substrate phosphorylation by Akt.{25455} It inhibits Akt1, 2, and 3 with IC50 values of 3, 7, and 7 nM, respectively and also inhibits P70S6K and PKA with similar potency (IC50s = 6 and 7 nM, respectively).{25455} Furthermore, AZD 5363 shows >75% inhibition at 1 μM against ROCK-II, MKK1, MSK1, MSK2, PKCγ, PKGα, PKGβ, PRKX, RSK2, and RSK3.{25455} At 3 μM or less, AZD 5363 has been reported to inhibit the proliferation of 41 out of 182 solid and hematologic tumor cell lines, demonstrating the greatest sensitivity towards breast cancer derived-cells or those with PIK3CA and/or PTEN mutations.{25455} Oral dosing to nude mice bearing BT474c xenografts resulted in antitumor activity, including the reduction of the phosphorylation of PRAS40, GSK3β, and S6 at an EC50 value of ~ 0.1 μM.{25455}
Brand:CaymanSKU:- Akt functions as a key component in multiple signaling pathways including those related to cell proliferation, metabolism, and survival as well as angiogenesis. AZD 5363 is a pyrrolopyrimidine-derived compound that inhibits Akt by competitively binding to the kinase domain, preventing substrate phosphorylation by Akt.{25455} It inhibits Akt1, 2, and 3 with IC50 values of 3, 7, and 7 nM, respectively and also inhibits P70S6K and PKA with similar potency (IC50s = 6 and 7 nM, respectively).{25455} Furthermore, AZD 5363 shows >75% inhibition at 1 μM against ROCK-II, MKK1, MSK1, MSK2, PKCγ, PKGα, PKGβ, PRKX, RSK2, and RSK3.{25455} At 3 μM or less, AZD 5363 has been reported to inhibit the proliferation of 41 out of 182 solid and hematologic tumor cell lines, demonstrating the greatest sensitivity towards breast cancer derived-cells or those with PIK3CA and/or PTEN mutations.{25455} Oral dosing to nude mice bearing BT474c xenografts resulted in antitumor activity, including the reduction of the phosphorylation of PRAS40, GSK3β, and S6 at an EC50 value of ~ 0.1 μM.{25455}
Brand:CaymanSKU:- Akt functions as a key component in multiple signaling pathways including those related to cell proliferation, metabolism, and survival as well as angiogenesis. AZD 5363 is a pyrrolopyrimidine-derived compound that inhibits Akt by competitively binding to the kinase domain, preventing substrate phosphorylation by Akt.{25455} It inhibits Akt1, 2, and 3 with IC50 values of 3, 7, and 7 nM, respectively and also inhibits P70S6K and PKA with similar potency (IC50s = 6 and 7 nM, respectively).{25455} Furthermore, AZD 5363 shows >75% inhibition at 1 μM against ROCK-II, MKK1, MSK1, MSK2, PKCγ, PKGα, PKGβ, PRKX, RSK2, and RSK3.{25455} At 3 μM or less, AZD 5363 has been reported to inhibit the proliferation of 41 out of 182 solid and hematologic tumor cell lines, demonstrating the greatest sensitivity towards breast cancer derived-cells or those with PIK3CA and/or PTEN mutations.{25455} Oral dosing to nude mice bearing BT474c xenografts resulted in antitumor activity, including the reduction of the phosphorylation of PRAS40, GSK3β, and S6 at an EC50 value of ~ 0.1 μM.{25455}
Brand:CaymanSKU:-