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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 )
配置溶液
溶液 1
30% propylene glycol, 5% Tween 80, 65% D5W: 20 mg/mL
icon Note
For research use only .
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Amily
