837364-57-5
837364-57-5 structure
- Name: AG-024322
- Chemical Name: N-[[5-[(3E)-3-(4,6-difluorobenzimidazol-2-ylidene)-1,2-dihydroindazol-5-yl]-4-methylpyridin-3-yl]methyl]ethanamine
- CAS Number: 837364-57-5
- Molecular Formula: C23H20F2N6
- Molecular Weight: 418.44200
- Catalog: Signaling Pathways Immunology/Inflammation COX
- Create Date: 2018-08-01 20:57:49
- Modify Date: 2024-09-17 18:08:55
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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[1]. AG-024322 displays broad-spectrum anti-tumor activity and clear target modulation in vivo. AG-024322 induces cell apoptosis[3].
| Name | N-[[5-[(3E)-3-(4,6-difluorobenzimidazol-2-ylidene)-1,2-dihydroindazol-5-yl]-4-methylpyridin-3-yl]methyl]ethanamine |
|---|---|
| Synonyms | unii-926f8x7tno |
| Description | 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[1]. AG-024322 displays broad-spectrum anti-tumor activity and clear target modulation in vivo. AG-024322 induces cell apoptosis[3]. |
|---|---|
| Related Catalog | |
| Target |
COX-1:2.3 nM (Ki) COX-2:3 nM (Ki) COX-4:2.9 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]. 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]. |
| 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) 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]. Animal Model: Male and female cynomolgus monkeys[1] Dosage: 2, 6, and 10 mg/kg (Toxicity analysis) Administration: Intravenous infusion; 5 days Result: Resulted in dose-dependent pancytic bone marrow hypocellularity and lymphoid depletion in lymph nodes, spleen, and/or thymus at >6 mg/kg. |
| References |
| Molecular Formula | C23H20F2N6 |
|---|---|
| Molecular Weight | 418.44200 |
| Exact Mass | 418.17200 |
| PSA | 81.22000 |
| LogP | 1.81600 |
| Hazard Codes | Xi |
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