PHA-793887

PHA‑793887 is a potent small molecule inhibitor of multiple cyclin-dependent kinases (CDKs), including CDK2 (IC50 = 8 nM), CDK1 (60 nM), CDK4 (62 nM), CDK5 (5 nM), and CDK7 (10 nM). It also inhibits glycogen synthase kinase 3β. Developed for intravenous administration as an anti-cancer agent targeting cell cycle regulation and proliferation pathways in solid tumors and leukemia. The drug was investigated in phase I clinical trials for advanced/metastatic solid tumors but development was halted due to severe dose-related hepatotoxicity. Mechanistically it induces cell-cycle arrest by inhibiting phosphorylation of key proteins such as Rb and nucleophosmin and modulates E2F gene signatures relevant to tumor growth suppression[1][2][3][4][5][7].

Other names

3-Methyl-N-[1,4,5,6-tetrahydro-6,6-dimethyl-5-[(1-methyl-4-piperidinyl)carbonyl]pyrrolo[3,4-c]pyrazol-3-yl]butanamideN-(6,6-dimethyl-5-(1-methylpiperidine-4-carbonyl)-1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazol-3-yl)-3-methylbutanamideUNII-MKS45S912BUNII-MKS-45S912BUNII-MKS 45S912B718630–59–2