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氨基酸及其衍生物 抑制剂 常见氨基酸及蛋白质类药
CP466722
发布者:信康   浏览次数:
  • 产品名称:CP466722
  • CAS:1080622-86-1
  • 别名:1-(6,7-二甲氧基-4-喹唑啉基)-3-(2-吡啶基)-1H-1,2,4-三唑-5-胺;CP-466722;CP466722
  • 英文名:CP466722
    • 密度 1.48
    • 储存条件 2-8°C
    • 溶解度 DMSO: soluble0.5mg/mL, clear (warmed)
    • 颜色white to beige
    • 生物活性CP-466722是一种有效的,可逆的ATM抑制剂,不影响ATR,且抑制PI3K或PIKK家族成员。
    • 体外研究In vitro, CP-466722 is identified as a potential inhibitor to decrease the activity of purified ATM kinase to phosphorylate GST-p53(1–101) substrate. In addition, CP-466722 also shows the inhibitory activities against abl and src kinases. In HeLa cells, CP-466722 at doses of 6μM, results in the inhibition in ATM-dependent phosphorylation by reversibly inhibiting ionizing radiation (IR)-induced ATM kinase activity. Besides, ATM-dependent p53 induction is also inhibited by CP-466722 in MCF-7 human breast cancer cells and primary and immortalized diploid human fibroblasts. In response to IR, CP-466722 increased proportion of cells with G2/M DNA content and reduces proportion of cells with G1-phase DNA content in HeLa cells. Transient exposure to CP-466722 for a period of 4 hours sensitizes HeLa cells to IR without affecting cell plating nor cell viability.