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AG-024322  ≥98%

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包装规格：1mg 5mg in glass bottle
产品描述：基本信息 产品编号： A11306 产品名称： AG-024322 CAS: 837364-57-5   储存条件 粉末 -20℃ 四年     分子式： C23H20F2N6 溶于液体 -80℃ 六个月 分子量 418.44 -20℃ 一个月 化学名：  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   生物活性 产品描述 一种有效的ATP竞争性的pan-CDK抑制剂，抑制CDK1，CDK2，CDK4的Ki值在1-3nM范围内。AG-024322在体内表现出广谱抗肿瘤活性和清晰的靶标调控。AG-024322诱导细胞凋亡(apoptosis)。 靶点 COX-1 2.3nM(Ki) COX-2 3nM(Ki) COX-4 2.9nM(Ki) 体外研究 AG-024322 (0.1-30μM; 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 AG-024322 (0-120nM) exhibits growth inhibition effects on HCT-116 cells. It is slightly less potent in the functional cellular assay with an IC50 of 120nM 体内研究 AG-024322 (intravenous infusion; 2, 6, and 10mg/kg; 5 days) exhibits no-adverse-effect at 2mg/kg with mean plasma AUC (0- 24.5) of 2.11 g.h/mL. At 6mg/kg produces pancytic bone marrow hypocellularity, lymphoid depletion. And vascular injury at the injection site renal tubular degeneration occurs at 10mg/kg AG-024322 (20mg/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 AG-024322 (20mg/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 Animal Model: Male and female cynomolgus monkeys Dosage: 2, 6, and 10mg/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 >6mg/kg.
保存条件：-20℃

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