R547 is a potent, selective and ATP-competitive CDK inhibitor with Ki of 1/3/1 nM for CDK1/2/4, respectively.
R547 has no activity against a large panel of serine/threonine and tyrosine kinases.
R547 inhibits the growth of various human tumor cell lines (HCT116 cell line IC50=80 nM), blocks G1 and G2 phases, induces apoptosis and reduces phosphorylation of Rb.
R547 demonstrates significant in vivo efficacy in the HCT116 human colorectal tumor xenograft model in nude mice.
