Milciclib (PHA-848125)

Description: Milciclib (formerly also known as PHA-848125) is a novel, potent, ATP-competitive small molecule CDK inhibitor for CDK2 with IC50 of 45 nM. It is > 3-fold more selective for CDK2 than CDK1, 2, 4, 5, and 7. It is also an inhibitor of Tropomyosin receptor kinase (TRK), with IC50 of 53 nM. In cells treated with PHA-848125, hyperphosphorylated form of CDK substrate—retinoblastoma protein (pRb) was reduced and hypophosporylated from of pRb was accumulated. It further indicated inhibition effect of PHA-848125 on CDK2 activity.

References: J Med Chem. 2009 Aug 27; 52(16):5152-63; Mol Cancer Ther. 2010 Mar; 9(3):673-81.