Drug intelligence / Profile preview

ag-024322

Development stage
Unknown
Lead developer
Pfizer
Modality
Small Molecules
Administration
Intravenous
01

Overview

AG‑024322 is a potent, ATP‑competitive small molecule inhibitor of cyclin-dependent kinases (CDKs), specifically targeting CDK1, CDK2, and CDK4 with high selectivity and nanomolar potency. By inhibiting these kinases—key regulators of cell cycle progression—AG‑024322 induces cell cycle arrest, apoptosis, and inhibits DNA replication and tumor cell proliferation. The compound has demonstrated antiproliferative activity in multiple human tumor cell lines and antitumor effects in preclinical models. Developed by Agouron (Pfizer) as an intravenous anticancer agent for the treatment of neoplasms including lymphoma (non-Hodgkin), its clinical development reached phase I before being discontinued[1][3][4][5][7].

Other names
3-Pyridinemethanamine, 5-(3-(4,6-difluoro-1H-benzimidazol-2-yl)-1H-indazol-5-yl)-N-ethyl-4-methyl-UNII-926F8X7TNOUNII926F8X7TNOUNII 926F8X7TNO837364–57–5
02

Targets

UGT1A1 (UDP-glucuronosyltransferase 1A1)CDK2 (Cyclin-dependent kinase 2)CDK1 (Cyclin-dependent kinase 1)CDK4 (Cyclin-dependent kinase 4)

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