Simurosertib

Cdc7激酶抑制剂(IC50=0.26nM)；对Cdc7的选择性优于Cdk2和ROCK1（IC50s分别为6,300和430nM）；抑制HeLa细胞中MCM2的磷酸化(IC50=17nM)；降低COLO205细胞的增殖(EC50=81nM)；抑制多种癌细胞的生长(GI50s=30.2->10,000nM)；以80mg/kg的剂量降低COLO 205和SW948小鼠异种移植模型中肿瘤内磷酸化MCM2的水平，以40或60mg/kg的剂量每天两次给药时，可降低相同模型中的肿瘤生长。An inhibitor of Cdc7 kinase (IC50 = 0.26 nM); selective for Cdc7 over Cdk2 and ROCK1 (IC50s = 6,300 and 430 nM, respectively); inhibits phosphorylation of MCM2 in HeLa cells (IC50 = 17 nM); reduces proliferation of COLO 205 cells (EC50 = 81 nM); inhibits the growth of a wide variety of cancer cells (GI50s = 30.2->10,000 nM); reduces intratumor levels of phosphorylated MCM2 in COLO 205 and SW948 mouse xenograft models at 80 mg/kg and reduces tumor growth in the same models when administered at doses of 40 or 60 mg/kg twice per day.分子式C17H19N5OS分子量341.4O=C1N=C(NC2=C1SC(C3=CNN=C3C)=C2)[C@@]4([H])N5CCC(CC5)C4