AG-024322 MedChemExpress (MCE)

Product Name	AG-024322
Synonyms	CS-1092 AG024322 AG-24322 AG-024322 AG-024322 5-[3-(5,7-difluoro-1H-benzimidazol-2-yl)-1H-indazol-5-yl]-N-ethyl-4-methyl-3-Pyridinemethanamine 3-Pyridinemethanamine, 5-[3-(5,7-difluoro-1H-benzimidazol-2-yl)-1H-indazol-5-yl]-N-ethyl-4-methyl- Synonyms CS-1092 AG024322 AG-24322 AG-024322 AG-024322 5-[3-(5,7-difluoro-1H-benzimidazol-2-yl)-1H-indazol-5-yl]-N-ethyl-4-methyl-3-Pyridinemethanamine 3-Pyridinemethanamine, 5-[3-(5,7-difluoro-1H-benzimidazol-2-yl)-1H-indazol-5-yl]-N-ethyl-4-methyl- N-((5-((19E)-3-(4,6-DIFLUORO-2H-BENZO[D]IMIDAZOL-2-YLIDENE)-2,3-DIHYDRO-1H-INDAZOL-5-YL)-4-METHYLPYRIDIN-3-YL)METHYL)ETHANAMINE
CAS	837364-57-5
EINECS
Chemical Formula	C23H20F2N6
Molecular Weight	418.44
inchi
Package	10 mM * 1 mL;1 mg;5 mg
Price	Email to quote
Descriptions	AG-024322 AG-024322 MedChemExpress (MCE) HY-15491 837364-57-5 98.53% Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Room temperature in continental US Descriptions AG-024322 AG-024322 MedChemExpress (MCE) HY-15491 837364-57-5 98.53% Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Room temperature in continental US may vary elsewhere. AG-024322 is a potent ATP-competitive pan-CDK inhibitor against cell cycle kinases CDK1, CDK2, and CDK4 with Ki values in the 1-3 nM range. AG-024322 displays broad-spectrum anti-tumor activity and clear target modulation in vivo. AG-024322 induces cell apoptosis. AG-024322 (0.1-30 μM 24 hours) is less toxic at concentrations below 3 μM, the viability of human PBMCs as measured by ATP content with a TC50 value of 1.4 μM for human PBMCs[2].AG-024322 (0-120 nM) exhibits growth inhibition effects on HCT-116 cells. It is slightly less potent in the functional cellular assay with an IC50 of 120 nM[2]. AG-024322 (intravenous infusion 2, 6, and 10 mg/kg 5 days) exhibits no-adverse-effect at 2 mg/kg with mean plasma AUC (0-24.5) of 2.11 g.h/mL. At 6 mg/kg produces pancytic bone marrow hypocellularity, lymphoid depletion. And vascular injury at the injection site renal tubular degeneration occurs at 10 mg/kg[1].AG-024322 (20 mg/kg) inhibits the growth of established human tumor xenografts of different origins with tumor growth inhibition (TGI) ranging from 32% to 86.4%.It also exhibits anti-tumor effects as a dose-pdependent manner[3].AG-024322 (20 mg/kg) causes a 65% TGI in the MV522 tumor model. It results a 52% TGI at 1/2 of the maximum tolerated dose (MTD) and only slight anti-tumor activity at 1/4 of the MTD[3]. COX-1 2.3 nM (Ki) COX-2 3 nM (Ki) COX-4 2.9 nM (Ki) \| \| \| \| \| \| \| \| \| \| [1]. Brown AP, et al. Toxicity and toxicokinetics of the cyclin-dependent kinase inhibitor AG-024322 in cynomolgus monkeys following intravenous infusion.Cancer Chemother Pharmacol. 2008 Nov 62(6):1091-101. [Content Brief] [2]. Jessen BA,et al. Peripheral white blood cell toxicity induced by broad spectrum cyclin-dependent kinase inhibitors.J Appl Toxicol. 2007 Mar-Apr 27(2):133-42. [Content Brief] [3]. Cathy C. Zhang, et al. AG-024322 is a multi-targeted CDK inhibitor with potent antitumor activity in vivo. Cellular and Molecular Biology 53: Cell Cycle Control and Cancer 1
Last Update	2025-04-01 14:45:47

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