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Sunitinib (Sutent) is a multitargeted FLT3, PDGFRs, VEGFRs, and Kit kinase inhibitor with Ki of 0.009 and 0.008 µM for Flk-1 and PDGFR, respectively. In RS4;11 cells (FLT3-WT), addition of FL was necessary to stimulate FLT3 phosphorylation, and treatment with SU11248 inhibited FLT3-WT phosphorylation in a dose-dependent manner with a 50% inhibitory concentration of approximately 250 nM. In MV4;11 cells that express FLT3-ITD, it is noteworthy that both high and low molecular weight forms of FLT3 are phosphorylated in the absence of FLT3 ligand (FL), consistent with expression of FLT3-ITD. Sunitinib Malate (Sutent, SU11248) inhibited FLT3-ITD phosphorylation in a dose-dependent manner with an IC50 of 50 nM following a 2-hour treatment. Evaluating the ability of Sunitinib (Sutent) to inhibit ligand-dependent receptor phosphorylation in cells, the effect of sunitinib (Sutent) on ligand-dependent proliferation of cells was examined. Sunitinib (Sutent) inhibited VEGF- and FGF-induced proliferation of HUVECs with IC50 of 0.04 and 0.7 µM, respectively. Sunitinib (Sutent) also inhibited PDGF-induced proliferation of NIH-3T3 cells overexpressing PDGFR¦Á or PDGFR¦Â with IC50 of 0.03 and 0.07 µM, respectively.

June 21, 2017

prudect name : Sunitinib (Sutent) is a multitargeted FLT3, PDGFRs, VEGFRs, and Kit kinase inhibitor with Ki of 0.009 and 0.008 µM for Flk-1 and PDGFR, respectively. In RS4;11 cells…

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Sorafenib tosylate is the first listing of approved drugs targeting multiple targets, but also over the past decade is the only FDA approved drug for the treatment of renal cell carcinoma.

prudect name : Sorafenib tosylate is the first listing of approved drugs targeting multiple targets, but also over the past decade is the only FDA approved drug for the treatment…

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SGI-7079 is an Axl inhibitor, significantly inhibits the proliferation of SUM149 or KPL-4 cells with an IC50 of 0.43 or 0.16 ¦ÌM, respectively.

prudect name : SGI-7079 is an Axl inhibitor, significantly inhibits the proliferation of SUM149 or KPL-4 cells with an IC50 of 0.43 or 0.16 ¦ÌM, respectively.SGI 7079 Synonyms: CAS NO:…

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6-(2,4-Difluorophenoxy)-8-methyl-2-[(tetrahydro-2H-pyran-4-yl)amino]pyrido[2,3-d]pyrimidin-7(8H)-one hydrochloride

prudect name : 6-(2,4-Difluorophenoxy)-8-methyl-2-[(tetrahydro-2H-pyran-4-yl)amino]pyrido[2,3-d]pyrimidin-7(8H)-one hydrochlorideSY-R1487;R1487 Synonyms: CAS NO: 449808-64-4Molecular Formula: C19H18F2N4O3.HClMolecular Weight: 424.83Purity: 98% minSolubility: In DMSOStorage: -20 oC web site: www.medchemexpress.com

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SGX523 is a novel, ATP-competitive kinase inhibitor remarkable for its exquisite selectivity for MET. SGX523 potently inhibited MET with an IC50 of 4 nmol/L and is >1,000-fold selective versus the >200-fold selectivity of other protein kinases tested in biochemical assays. Crystallographic study revealed that SGX523 stabilizes MET in a unique inactive conformation that is inaccessible to other protein kinases, suggesting an explanation for the selectivity. SGX523 inhibited MET-mediated signaling, cell proliferation, and cell migration at nanomolar concentrations but had no effect on signaling dependent on other protein kinases, including the closely related RON, even at micromolar concentrations. SGX523 inhibition of MET in vivo was associated with the dose-dependent inhibition of growth of tumor xenografts derived from human glioblastoma and lung and gastric cancers, confirming the dependence of these tumors on MET catalytic activity. Our results show that SGX523 is the most selective inhibitor of MET catalytic activity described to date and is thus a useful tool to investigate the role of MET kinase in cancer without the confounding effects of promiscuous protein kinase inhibition.

prudect name : SGX523 is a novel, ATP-competitive kinase inhibitor remarkable for its exquisite selectivity for MET. SGX523 potently inhibited MET with an IC50 of 4 nmol/L and is >1,000-fold…

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(5Z)-5-[[3-(Trifluoromethyl)phenyl]methylene]-2,4-thiazolidinedione;TCS PIM-1 4a;SMI-4a

prudect name : (5Z)-5-[[3-(Trifluoromethyl)phenyl]methylene]-2,4-thiazolidinedione;TCS PIM-1 4a;SMI-4aSMI-4a Synonyms: CAS NO: 438190-29-5 327033-36-3 Molecular Formula: C11H6F3NO2SMolecular Weight: 273.23Purity: 98% minSolubility: In DMSOStorage: −20°C web site: www.medchemexpress.com

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SNS-314 Mesylate is a potent and selective inhibitor of Aurora A, Aurora B and Aurora C with IC50 of 9 nM, 31 nM, and 3 nM, respectively. It is less potent to Trk A/B, Flt4, Fms, Axl, c-Raf and DDR2. Phase 1.

prudect name : SNS-314 Mesylate is a potent and selective inhibitor of Aurora A, Aurora B and Aurora C with IC50 of 9 nM, 31 nM, and 3 nM, respectively….

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Saxagliptin is a dipeptidyl peptidase – ¢ô inhibitor,New treatment of type 2 diabetes.

prudect name : Saxagliptin is a dipeptidyl peptidase – ¢ô inhibitor,New treatment of type 2 diabetes.Saxagliptin hydrate Synonyms: CAS NO: 945667-22-1Molecular Formula: C18H25N3O2 . H2OMolecular Weight: 333.43Purity: 99%Solubility: Storage: −20°C…

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prudect name : SRT3109Synonyms: CAS NO: 1204707-71-0Molecular Formula: C18H23F2N5O4S2Molecular Weight: 475.54Purity: 98% minSolubility: In DMSOStorage:

prudect name : SRT3109 Synonyms: CAS NO: 1204707-71-0Molecular Formula: C18H23F2N5O4S2Molecular Weight: 475.54Purity: 98% minSolubility: In DMSOStorage: −20°C web site: www.medchemexpress.com

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Siramesine(Lu 28-179) Hcl is a selective sigma-2 receptor agonist, which has been shown to trigger cell death of cancer cells and to exhibit a potent anticancer activity in vivo.

prudect name : Siramesine(Lu 28-179) Hcl is a selective sigma-2 receptor agonist, which has been shown to trigger cell death of cancer cells and to exhibit a potent anticancer activity…

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