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AG-024322

CAS No. : 837364-57-5

MCE 站：AG-024322

产品活性：AG-024322 是一种有效的 ATP 竞争性的 pan-CDK 抑制剂，抑制 CDK1， CDK2， CDK4 的 K_i 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)。

研究领域：Immunology/Inflammation  |  Apoptosis

作用靶点：COX  |  Apoptosis

In Vitro: AG-024322 (0.1-30 μM; 24 hours) is less toxic at concentrations below 3 ?M, the viability of human PBMCs as measured by ATP content with a TC₅₀ value of 1.4 ?M for human PBMCs.
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.

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.
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.
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.

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