Powder: -20°C for 3 years | In solvent: -80°C for 1 year
KU-0060648 是一种 PI3K 和 DNA-PK 的双重抑制剂,对 PI3Kα、PI3Kβ、PI3Kδ、PI3Kγ 和 DNA-PK 的 IC50值分别为 4 nM、0.5 nM、0.1 nM、0.59 nM 和 8.6 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 472 | 现货 | ||
5 mg | ¥ 1,070 | 现货 | ||
10 mg | ¥ 1,730 | 现货 | ||
25 mg | ¥ 3,150 | 现货 | ||
50 mg | ¥ 4,520 | 现货 | ||
100 mg | ¥ 6,350 | 现货 |
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 | PI3Kα:4 nM, PI3Kβ:0.5 nM, PI3Kδ:0.1 nM |
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] |
细胞实验 | SRB assay(Only for Reference) |
别名 | KU0060648 |
分子量 | 582.71 |
分子式 | C33H34N4O4S |
CAS No. | 881375-00-4 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
2eq.HCl: 58.3 mg/mL (100 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
2eq.HCl | 1 mM | 1.7161 mL | 8.5806 mL | 17.1612 mL | 42.903 mL |
5 mM | 0.3432 mL | 1.7161 mL | 3.4322 mL | 8.5806 mL | |
10 mM | 0.1716 mL | 0.8581 mL | 1.7161 mL | 4.2903 mL | |
20 mM | 0.0858 mL | 0.429 mL | 0.8581 mL | 2.1451 mL | |
50 mM | 0.0343 mL | 0.1716 mL | 0.3432 mL | 0.8581 mL | |
100 mM | 0.0172 mL | 0.0858 mL | 0.1716 mL | 0.429 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
KU-0060648 881375-00-4 DNA Damage/DNA Repair PI3K/Akt/mTOR signaling DNA-PK PI3K mTOR inhibit Phosphoinositide 3-kinase KU0060648 Inhibitor Mammalian target of Rapamycin KU 0060648 DNA-dependent protein kinase inhibitor