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BAY-707

产品编号 T14509 CAS 2109805-96-9

BAY-707, a highly potent and selective substrate-competitive inhibitor of MTH1 (NUDT1) with an IC50 of 2.3 nM, is well-tolerated in mice and exhibits a favorable pharmacokinetic (PK) profile compared to other MTH1 compounds. However, it demonstrates a clear lack of anticancer efficacy both in vitro and in vivo[1].

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BAY-707, CAS 2109805-96-9

规格	价格/CNY		货期	数量
5 mg	￥ 2,380		35日内发货
25 mg	￥ 9,800		35日内发货

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其他形式的 BAY-707:

BAY-707 acetate
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生物活性

化学信息

存储 & 溶解度

参考文献

产品描述	BAY-707, a highly potent and selective substrate-competitive inhibitor of MTH1 (NUDT1) with an IC50 of 2.3 nM, is well-tolerated in mice and exhibits a favorable pharmacokinetic (PK) profile compared to other MTH1 compounds. However, it demonstrates a clear lack of anticancer efficacy both in vitro and in vivo[1].
靶点活性	MTH1/NUDT1:2.3 nM
体外活性	BAY-707 demonstrates a superior cellular target engagement with an EC50 of 7.6 nM, in agreement with its higher enzymatic potency (IC50=2.3 nM)[1] and it also demonstrates a high cell permeability cell permeability in the Caco-2 assay with a efflux ratio of 288 nm/s[1]. BAY-707 (0-30 μM; 24 hours) has no antiproliferative effects in HMEC, HeLa and SW-480 cells[1]. BAY-707 shows an overall favorable physicochemical profile and promising?in vitro?pharmacokinetic properties with high metabolic stability in both human microsomes(0.29L/h/kg,Fmax=78%) and rat hepatocytes (0.54L/h/kg,Fmax=87%)[1].
体内活性	BAY-707 (orally adminstation; 50-250 mg/kg; 2 weeks) is well-tolerated in nude mice, after 7-days treatment, body weight loss does not exceed 10% [1] and it also exhibits superior biochemical potency, cellular target engagement, and a pharmacokinetic profile to other MTH1 tool compounds. However, Bay-077 exerts no anticancer efficacy either in mono- or in combination therapies in CT26 and NCI-H460 mice model[1].

分子量	288.34
分子式	C15H20N4O2
CAS No.	2109805-96-9

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

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参考文献

1. Ellermann M, et al. Novel Class of Potent and Cellularly Active Inhibitors Devalidates MTH1 as Broad-Spectrum Cancer Target.ACS Chem Biol. 2017 Aug 18;12(8):1986-1992.

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

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。

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第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

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