| Identification | Back Directory | [Name]
AG-024322 | [CAS]
837364-57-5 | [Synonyms]
CS-1092
AG-24322
AG-024322
AG024322; 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 | [Molecular Formula]
C23H20F2N6 | [MDL Number]
MFCD11100348 | [MOL File]
837364-57-5.mol | [Molecular Weight]
418.44 |
| Chemical Properties | Back Directory | [Boiling point ]
668.4±65.0 °C(Predicted) | [density ]
1.361±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [form ]
Solid | [pka]
7.84±0.30(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
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]. | [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. |
| [IC 50]
COX-1: 2.3 nM (Ki); COX-2: 3 nM (Ki); COX-4: 2.9 nM (Ki) | [storage]
Store at -20°C | [References]
[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. DOI:10.1007/s00280-008-0771-1
[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. DOI:10.1002/jat.1177
[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 |
|
| Company Name: |
BOC Sciences
|
| Tel: |
1-631-485-4226; 16314854226 |
| Website: |
https://www.bocsci.com |
| Company Name: |
Cckinase, Inc.
|
| Tel: |
+1 (732)236-3202 |
| Website: |
www.cckinase.com |
| Company Name: |
cjbscvictory
|
| Tel: |
13348960310 13348960310; |
| Website: |
https://www.weikeqi-biotech.com/ |
| Company Name: |
Cellosaurus STR
|
| Tel: |
13121892008 |
| Website: |
www.cellosaurus.org |
|