Sunitinib Malate

Sunitinib Malate              
            上海义森生物科技有限公司技术数据:

分子量(MW):	532.56
化学式:	C22H27FN4O2.C4H6O5
溶解度:	DMSO 15mg/mL   Water <1mg/mL   Ethanol <1mg/mL
纯度:	>99%
稳定性:	at -20℃ 2 years
CAS号:	341031-54-7, 557795-19-4 (free base), 1126641-10-8 ( Maleic acid)

生物活性 
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 PDGFRα or PDGFRβ with IC50 of 0.03 and 0.07 µM, respectively. [1][2]