326823-27-2

PNU-292137 is an orally active, potent CDK2 inhibitor with IC50s of 37 nM and 92 nM for CDK2/cyclin A and CDK2/cyclin E, respectively. PNU-292137 makes interactions with the hydrophobic pocket at the back of the CDK2 ATP pocket. PNU-292137 efficiently inhibits tumor cell proliferation in human colon and prostate tumor cell lines. PNU-292137 exhibits antitumor activity (TGI>50%) in a mouse xenograft model[1].

CDK2/cyclinA: 37 nM (IC₅₀); CDK2/cyclin E: 92 nM (IC₅₀); Cdk5/p25: 114 nM (IC₅₀); CDK1/cyclinB: 270 nM (IC₅₀); CDK4/cyclinD1: >10000 nM (IC₅₀); GSK-3β: 1905 nM (IC₅₀); ERK-2: 4600 nM (IC₅₀)

[1] Paolo Pevarello, et al. 3-Aminopyrazole inhibitors of CDK2/cyclin A as antitumor agents. 1. Lead finding. J Med Chem. 2004 Jun 17;47(13):3367-80. DOI:10.1021/jm031145u