KU 59403|845932-30-1|-陌孚医药/Medlife

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KU 59403

目录号: PL04821 纯度: ≥98%

CAS No. :845932-30-1

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中文名称	KU 59403
中文别名	化合物 T15673
英文名称	KU 59403
英文别名	1-Piperazinepropanamide, 4-methyl-N-[6-[6-(4-morpholinyl)-4-oxo-4H-pyran-2-yl]-2-thianthrenyl]-;KU59403;KU 59403;BCP28847;3-(4-Methylpiperazin-1-yl)-N-[6-(6-morpholin-4-yl-4-oxopyran-2-yl)thianthren-2-yl]propanamide;3-(4-methylpiperazin-1-yl)-N-(6-(6-morpholino-4-oxo-4H-pyran-2-yl)thianthren-2-yl)propanamide.;BDBM50378201;CID 11433009
Cas No.	845932-30-1
分子式	C₂₉H₃₂N₄O₄S₂
分子量	564.72
包装储存	-20°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

产品详情	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。
生物活性	KU 59403 is a potent ATM inhibitor, with IC 50 values of 3 nM, 9.1 μM and 10 μM for ATM, DNA-PK and PI3K, respectively.
性状	Solid
IC50 & Target[1][2]	IC50: 3 nM (ATM).
体外研究(In Vitro)	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. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)	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. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	-20°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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.

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1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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