AG-024322

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AG-024322  纯度: 98.69%

AG-024322 是一种有效的 ATP 竞争性的 pan-CDK 抑制剂，抑制 CDK1， CDK2， CDK4 的 Ki 值在 1-3 nM 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)。

AG-024322

AG-024322 Chemical Structure

CAS No. : 837364-57-5

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5 mg ￥6000 In-stock
10 mg ￥9800 In-stock
25 mg ￥19500 In-stock
50 mg ￥31000 In-stock
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AG-024322 相关产品

•相关化合物库:

  • Clinical Compound Library Plus
  • Bioactive Compound Library Plus
  • Apoptosis Compound Library
  • Immunology/Inflammation Compound Library
  • Kinase Inhibitor Library
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生物活性

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].

IC50 & Target[1]

COX-1

2.3 nM (Ki)

COX-2

3 nM (Ki)

COX-4

2.9 nM (Ki)

体外研究
(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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

Clinical Trial

分子量

418.44

Formula

C23H20F2N6
CAS 号

837364-57-5
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
参考文献

  • [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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