Sunitinib

货号：S6761

储存条件：粉末-20°C可保存3年；液体-80°C可保存12月。

 

产品描述

VEGFR (vascular endothelial growth factor) and PDGFR (platelet-derived growth factor receptor) are critical roles in tumor growth and suvival via autocrine and paracrine loops, making them the well validated targets for the treatment of cancers. Sunitinib is a multiple RTKs inhibitor with IC50 values of 2nM and 80nM for VEGFR2 and PDGFRβ (measured by kinase activity), respectively, also shows inhibition against KIT and FLT3 receptor. The cellular kinase activity induced by VEGF/PDGF can be inhibited by Sunitinib with IC50 value of 5-50nM/10nM in 3T3 cells, while the PDGF-induced cell growth can be inhibited by Sunitinib with IC50 of 8nM. Daily oral administration of Sunitinib at dose of 80mg/kg reduced growth of established SF763T tumor xenografts in athymic mice, as well as suppressed Colo205 tumor growth. Consistent with the cellular kinase study, the inhibition by Sunitinib against p-PDGFRβ can be observed in tumor after a single dose at 80mg/kg in mice bearing SF767T tumors and mice bearing Colo205 tumors, as well as suppressed p-FLK1 in A375 xenograft mice dosed 40mg/kg Sunitinib.

 

作用机制
Sunitinib is an ATP-competitive multitargeted tyrosine kinase inhibitor.

 

产品信息

CAS号	557795-19-4
分子式	C22H27FN4O2
分子量	398.47
别名	SU-11248
溶解度	DMSO	10.0 mg/mL (25.1 mM) warming
	Water	insoluble