CDK2 Inhibitor AVZO-021

**Semantic type:** Pharmacologic Substance

**Definition:** An orally bioavailable inhibitor of cyclin-dependent kinase 2 (CDK2), with potential antineoplastic activity. Upon oral administration, CDK2 inhibitor AVZO-021 selectively targets, reversibly binds to and inhibits the activity of the CDK2/CyclinE1 (CCNE1; CCNE-1) complex. This inhibits retinoblastoma (Rb) phosphorylation and blocks G1/S transition, which leads to cell cycle arrest, the induction of apoptosis, and the inhibition of proliferation in CDK2 and/or CCNE1-overexpressing tumor cells. 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. CCNE1, a regulatory factor and activator of CDK2 is overexpressed in various tumor cell types and CCNE1 overexpression elevates the activity of CDK2.

**Synonyms:** - ARTS 021 - ARTS-021 - ARTS021 - AVZO 021 - AVZO-021 - AVZO021 - CDK2 Inhibitor ARTS-021