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  • 产品名称: KU0060648
  • 产品货号: CS6557
  • 货期: 现货
  • 价格与订购: 1000
  • 数量:
    库存: 100
  • 规格: 1mg 2mg 10mg
  • 产品信息
  • 如何订购
    产品描述
    KU-0060648 is a dual inhibitor of DNA-PK and PI3Kα, PI3Kβ, PI3Kδ with IC50 of 8.6 nM and 4 nM, 0.5 nM, 0.1 nM respectively, less inhibition of PI3Kγ with IC50 of 0.59 μM.
    靶点活性
    DNA-PK    PI3Kα    PI3Kβ    PI3Kγ    PI3Kδ
    体外活性
    KU-0060648 exhibits differential effects on growth inhibition, but is not profoundly cytotoxic in a panel of human cancer cell lines. It inhibits DNA-PK and PI-3K with greater potency in MCF7 than SW620 cell using cell-based assays. Five-day exposure to 1 mM KU-0060648 inhibits cell proliferation by more than 95% in MCF7 cells but only by 55% in SW620 cells. In clonogenic survival assays, KU-0060648 increases the cytotoxicity of etoposide and doxorubicin across the panel of DNA-PKcs-proficient cells, but not in DNA-PKcs-deficient cells, confirming that enhanced cytotoxicity of the topoisomerase II poisons etoposide and doxorubicin is due to DNA-PK inhibition. [1]
    体内活性
    KU-0060648 enhances the anti-tumour activity of etoposide in both MCF7 and SW620 xenograft models, and has single-agent activity in the MCF7 xenograft model. [1]icon
    细胞实验
    SRB assay(Only for Reference) Cell lines: MCF7, T47D, MDA-MB-231, LoVo and SW620icon
    参考文献
    1. Munck JM, et al. Mol Cancer Ther, 2012, 11(8), 1789-1798.
    2. Celine Cano, et al. Mol Cancer Ther, 2009, 8(12 Suppl), A138.
    3. Chen MB, et al. KU-0060648 inhibits hepatocellular carcinoma cells through DNA-PKcs-dependent and DNA-PKcs-independent mechanisms. Oncotarget. 2016 Mar 29;7(13):17047-59.
    别名
    KU 0060648 , KU-0060648 , KU-0060648 KU 0060648
    纯度
    98.0%
    分子量
    582.71
    分子式
    C33H34N4O4S
    CAS No
    881375-00-4
    存储
    0-4℃ for short term (days to weeks), or -20℃ for long term (months).
    溶解度
    2eq.HCl: 58.3 mg/mL (100 mM)
    ( < 1 mg/ml refers to the product slightly soluble or insoluble )
    icon
    配置溶液
    溶液 1
    30% propylene glycol, 5% Tween 80, 65% D5W: 20 mg/mL
    icon
    Note
    For research use only .