Savolitinib

c-Met抑制剂(IC50=5nM)；1µM时选择性抑制274种其他激酶中的c-Met；抑制NCIH441人NSCLC细胞中的c-Met自身磷酸化(IC50=3nM)；抑制HGF诱导的NCIH441细胞生长(IC50=6nM)；抑制一组c-Met失调的胃癌细胞增殖(EC50s=0.6-14.7nM)；3mg/kg时抑制肿瘤内c-Met自身磷酸化94%并减缓Hs 746T人胃癌小鼠异种移植模型中的肿瘤生长。An inhibitor of c-Met (IC50 = 5 nM); selectivity inhibits c-Met over 274 other kinases at 1 µM; inhibits c-Met autophosphorylation in NCI H441 human NSCLC cells (IC50 = 3 nM); inhibits HGF-induced growth of NCI H441 cells (IC50 = 6 nM); inhibits proliferation in a panel of gastric cancer cells with dysregulated c-Met (EC50s = 0.6-14.7 nM); inhibits intratumor c-Met autophosphorylation by 94% and reduces tumor growth in a Hs 746T human stomach cancer mouse xenograft model at 3 mg/kg.分子式C17H15N9分子量345.4C[C@@H](C1=CN2C(C=C1)=NC=C2)N3C4=NC(C5=CN(C)N=C5)=CN=C4N=N3