Description
An inhibitor of Cdk2 and Cdk9 (IC50s = 4.5 and 20.5 nM, respectively); selective for Cdk2 and Cdk9 over Cdk1, -4, and -7 (IC50s = 278, 193, and 232 nM, respectively); inhibits the proliferation of COLO 205 cells (IC50 = 0.31 µM); inhibits proliferation in a panel of five breast cancer cell lines (IC50s = <0.4 µM for all); decreases phosphorylation of the RNA polymerase II C-terminal domain and RB and induces apoptosis in COLO 205 cells; reduces tumor volume in an EoL-1 mouse xenograft model at 40 and 55 mg/kg; inhibits tumor growth in an HL-60 mouse xenograft model at 70 mg/kg