中文名 | N-ethyl-4-[(3S)-3-methylmorpholin-4-yl]-1H-pyrrolo[2,3-b]pyridine-2-carboxamide |
英文名 | BAY-707 |
别名 | 化合物 T14509 |
英文别名 | BAY-707 BAY707) BAY-707(BAY 707 BAY-707 free base N-ethyl-4-[(3S)-3-methylmorpholin-4-yl]-1H-pyrrolo[2,3-b]pyridine-2-carboxamide 1H-Pyrrolo[2,3-b]pyridine-2-carboxamide, N-ethyl-4-[(3S)-3-methyl-4-morpholinyl]- |
CAS | 2109805-96-9 |
化学式 | C15H20N4O2 |
分子量 | 288.34 |
密度 | 1.225±0.06 g/cm3(Predicted) |
酸度系数 | 14.36±0.40(Predicted) |
存储条件 | 2-8°C,密封,干燥 |
体外研究 | BAY-707 demonstrates a superior cellular target engagement with an EC 50 of 7.6 nM, in agreement with its higher enzymatic potency (IC 50 =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 promisingin vitropharmacokinetic properties with high metabolic stability in both human microsomes(0.29L/h/kg,F max =78%) and rat hepatocytes (0.54L/h/kg,F max =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% . |
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