| Description |
A cell-permeable and metabolically stable (t 1/2 >30 min at 37 °C in the presence of rat liver microsomes, NADPH, and UDPGA) pyridinylmethylamino-isoquinoline dione that acts as a potent, ATP-binding site-targeting inhibitor against Cdk4/D1 kinase activity (IC 50 = 30 nM in cell-free Rb c-terminal fragment phosphorylation assays) and an effective antiproliferative agent against HCT116 colorectal and MCF-7 breast cancer cultures (IC 50 = 0.73 and 0.88 µM, respectively), while affecting Cdk2/E and Cdk1/B kinase activities only at much higher concentrations (IC 50 = 1.6 and 25.3 µM, respectively).
|
