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AG-024322

Catalog No. T14136   CAS 837364-57-5

AG-024322 is a potent ATP-competitive inhibitor of pan-CDK against cell cycle kinases CDK1, CDK2, and CDK4(Ki values in the 1-3 nM range)

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AG-024322 Chemical Structure
AG-024322, CAS 837364-57-5
Pack Size Availability Price/USD Quantity
25 mg 6-8 weeks $ 1,970.00
50 mg 6-8 weeks $ 2,580.00
100 mg 6-8 weeks $ 3,400.00
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Biological Description
Chemical Properties
Storage & Solubility Information
Description AG-024322 is a potent ATP-competitive inhibitor of pan-CDK against cell cycle kinases CDK1, CDK2, and CDK4(Ki values in the 1-3 nM range)
Targets&IC50 CDK2:3 nM (ki), CDK1:2.3 nM (ki), CDK4:2.9 nM (ki)
In vitro 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]. It is slightly less potent in the functional cellular assay with an IC50 of 120 nM[2]. AG-024322 (0-120 nM) exhibits growth inhibition effects on HCT-116 cells.
In vivo 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) 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]. 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% and it also exhibits anti-tumor effects as a dose-pdependent manner[3].
Molecular Weight 418.44
Formula C23H20F2N6
CAS No. 837364-57-5

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

TargetMolReferences and Literature

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. 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. 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

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Keywords

AG-024322 837364-57-5 Cell Cycle/Checkpoint CDK AG 024322 AG024322 inhibitor inhibit

 

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