CDK2 inhibitor INCB123667

An orally bioavailable inhibitor of cyclin-dependent kinase 2 (CDK2), with potential antineoplastic activity. Upon oral administration, CDK2 inhibitor INCB123667 selectively targets, binds to and inhibits the activity of CDK2. This inhibits retinoblastoma (Rb) phosphorylation and blocks G1/S transition, which leads to cell cycle arrest, the induction of apoptosis, and the inhibition of tumor cell proliferation. CDK2, in complex with cyclin E1 (CCNE1; CCNE-1), phosphorylates Rb, which leads to E2F target gene expression and G1 to S-phase cell cycle progression. CDK2 and CCNE1 are overexpressed in various tumor cell types.