苏尼替尼
CAS号 | 557795-19-4 | 货号 | BCP02336 |
中文名 | 苏尼替尼 | ||
英文名 | Sunitinib | ||
中文别名 | 舒尼替尼; | ||
英文别名 | SU-11248;SU 11248;SU11248;SU-011248;SU011248;SU 011248; | ||
分子式 | C22H27FN4O2 | 分子量 | 398.48 |
生物活性 | Sunitinib is a potent ATP-competitive inhibitor of VEGFR2 (Flk1) and PDGFRβ with Ki of 9 nM and 8 nM, respectively, displaying >10-fold higher selectivity for VEGFR2 and PDGFR than FGFR-1, EGFR, Cdk2, Met, IGFR-1, Abl, and src. In serum-starved NIH-3T3 cells expressing VEGFR2 or PDGFRβ, Sunitinib inhibits VEGF-dependent VEGFR2 phosphorylation and PDGF-dependent PDGFRβ phosphorylation with IC50 of 10 nM and 10 nM, respectively. Sunitinib inhibits VEGF-induced proliferation of serum-starved HUVECs with IC50 of 40 nM, and inhibits PDGF-induced proliferation of NIH-3T3 cells overexpressing PDGFRβ or PDGFRα with IC50 of 39 nM and 69 nM, respectively. SU11248 also has potent activity against wild-type FLT3 (FLT3-WT), FLT3-ITD, and FLT3 activation loop (FLT3-Asp835) mutants in phosphorylation assays. SU11248 inhibits FLT3-driven phosphorylation and induces apoptosis in vitro. In addition, SU11248 inhibits FLT3-induced VEGF production . | ||
上下游产品 | 341031-54-7(苏尼替尼苹果酸盐) | ||
信号通路 | Angiogenesis/Protein Tyrosine Kinase | ||
靶 点 | VEGFR |
结构式
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