Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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)
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 |
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 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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AG-024322 837364-57-5 Cell Cycle/Checkpoint CDK AG 024322 AG024322 inhibitor inhibit