Description
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