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 (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.
Sunitinib malate

Synonyms: SutentCAS NO: 341031-54-7Molecular Formula: C₂₂H₂₇FN₄O₂.C₄H₆O₅Molecular Weight: 532.56Purity: 99%Solubility: In DMSOStorage: −20°C 2 years

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