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KU 59403

CAS No. 845932-30-1

KU 59403 ( —— )

产品货号. M33395 CAS No. 845932-30-1

KU 59403 是 ATM 的一个有效抑制剂,其对 ATM、DNA-PK 和 PI3K 的 IC50 值分别为 3 nM、9.1 μM 和 10 μM。

纯度: >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
规格 价格/人民币 库存 数量
25MG ¥6897 有现货
50MG ¥9149 有现货
100MG ¥13541 有现货
500MG 获取报价 有现货
1G 获取报价 有现货

生物学信息

  • 产品名称
    KU 59403
  • 注意事项
    本公司产品仅用于科研实验,不得用于人体或动物的临床与诊断
  • 产品简述
    KU 59403 是 ATM 的一个有效抑制剂,其对 ATM、DNA-PK 和 PI3K 的 IC50 值分别为 3 nM、9.1 μM 和 10 μM。
  • 产品描述
    KU 59403 is a potent ATM inhibitor, with IC50 values of 3 nM, 9.1 μM and 10 μM for ATM, DNA-PK and PI3K, respectively.
  • 体外实验
    KU 59403 (1 μM) enhances VP-16 (1 μM) cytotoxicity to a similar extent in HCT116 and HCT116-N7 cells, and in the p53 mutant SW620 cells and human breast cancer cell line, MDAMB-231, sensitisation is 11.9±4.7 and 3.8±1.8-fold respectively. Inhibition of IR-induced ATM activity by KU 59403 (1 μM) is approximately 50% in MDA-MB231 cells and >50% in HCT116 cells that have low ATM expression and activity.Cell Viability Assay Cell Line:LoVo, HCT116 and SW620 (human colon cancer), and U2OS (human osteosarcoma) and MDA-MB-231 (human breast cancer) cells.Concentration:1 μM.Incubation Time:16 hours.Result:Had at least 1000 times greater specificity for ATM over other members of the PI3K family tested.Enhanced camptothecin cytotoxicity in both cell lines with greater enhancement being observed in the LoVo compared to the SW620 cells. Significantly enhanced the cytotoxicity of fixed concentrations of VP-16 (0.1 and 1 μM) or NSC 123127 (10 or 100 nM) in these cell lines, with greater enhancement of VP-16 in SW620 cells and of NSC 123127 in LoVo cells.
  • 体内实验
    KU59403 with a single daily dose of 12.5 mg/kg causes a significant sensitization.Increasing the dose of KU59403 to 25 mg/kg given twice daily results in the greatest chemo-sensitisation with a 3-fold increase in BMY-40481-induced tumour growth delay in both SW620 and HCT116-N7 xenografts, in the absence of a significantly increased toxicity.Animal Model:CD-1 nude mice implanted with SW620 or HCT116-N7 human cancer cell lines at 1×107 cells per animal s.c. (n=5 per group).Dosage:6, 12.5 and 25 mg/kg.Administration:I.P. twice daily (0 and 4 hours) and 12.5 mg/kg once daily.Result:Treatment with BMY-40481 alone causes a modest tumour growth delay of 4 days (time to RTV4=10.5 days). This delay is extended to 8.5 days when given with KU 59403 at 12.5 mg/kg i.p. twice daily for 5 days and 11.5 days (time to RTV4=18 days) when given with KU 59403 at 25 mg/kg i.p. twice daily for 5 days.
  • 同义词
    ——
  • 通路
    Cell Cycle/DNA Damage
  • 靶点
    ATM/ATR
  • 受体
    ATM/ATR
  • 研究领域
    ——
  • 适应症
    ——

化学信息

  • CAS Number
    845932-30-1
  • 分子量
    564.72
  • 分子式
    C29H32N4O4S2
  • 纯度
    >98% (HPLC)
  • 溶解度
    In Vitro:?DMSO 中的溶解度 : 10 mg/mL (17.71 mM; 超声助溶 (<60°C)
  • SMILES
    CN1CCN(CCC(=O)Nc2ccc3Sc4c(Sc3c2)cccc4-c2cc(=O)cc(o2)N2CCOCC2)CC1
  • 化学全称
    ——

运输与储存

  • 储存条件
    (-20℃)
  • 运输条件
    With Ice Pack
  • 稳定性
    ≥ 2 years

参考文献

1. Batey MA, et al. Preclinical evaluation of a novel ATM inhibitor, KU59403, in vitro and in vivo in p53 functional and dysfunctional models of human cancer. Mol Cancer Ther. 2013 Jun;12(6):959-67.?
产品手册
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