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BAY-707  ≥98%

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包装规格：5mg 10mg 25mg 50mg 100mg in glass bottle
产品简介：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。
靶点：IC50:2.3 nM (MTH1/NUDT1)
体外研究：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). BAY-707 demonstrates a high cell permeability cell permeability in the Caco-2 assay with a efflux ratio of 288 nm/s. 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%). BAY-707 (0-30 μM; 24 hours) has no antiproliferative effects in HMEC, HeLa and SW-480 cells.
体内研究：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. 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%.
保存条件：-20℃
注意事项：v

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