Definition

An orally bioavailable inhibitor of cyclin-dependent kinase 2 (CDK2), with potential antineoplastic activity. Upon oral administration, CDK2 inhibitor NKT3447 selectively targets, reversibly binds to and inhibits the activity of CDK2. This blocks G1/S cell cycle transition, which leads to cell cycle arrest, the induction of apoptosis, and the inhibition of tumor cell proliferation. CDK2, a serine/threonine kinase that plays an important role in the regulation of cell cycle progression and cellular proliferation, is overexpressed in certain tumor cells.