BAY-707

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

BAY-707 

BAY-707 是 MTH1(NUDT1) 的底物竞争性,高效选择性抑制剂,IC50 值 为 2.3 nM。 BAY-707 与其他 MTH1 化合物相比具有良好的药代动力学特征,并且在小鼠中具有良好的耐受性,但实验明显缺乏体外或体内抗癌功效。

BAY-707

BAY-707 Chemical Structure

CAS No. : 2109805-96-9

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生物活性

BAY-707 is a substrate-competitive, highly potent and selective inhibitor of MTH1(NUDT1) with an IC50 of 2.3 nM. BAY-707 has a good pharmacokinetic (PK) profile to other MTH1 compounds and is well-tolerated in mice, but shows a clear lack of in vitro or in vivo anticancer efficacy[1].

IC50 & Target

IC50:2.3 nM (MTH1/NUDT1)[1]

体外研究
(In Vitro)

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].
BAY-707 demonstrates a high cell permeability cell permeability in the Caco-2 assay with a efflux ratio of 288 nm/s[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].
BAY-707 (0-30 μM; 24 hours) has no antiproliferative effects in HMEC, HeLa and SW-480 cells[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

Bay-077 (orally adminstation; 50-250 mg/kg; 2 weeks) exhibits superior biochemical potency, cellular target engagement, and a pharmacokinetic profile to other MTH1 tool compounds, But Bay-077 exerts no anticancer efficacy either in mono- or in combination therapies in CT26 and NCI-H460 mice model[1].
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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

288.34

Formula

C15H20N4O2

CAS 号

2109805-96-9

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

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.

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