BAY707)
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- CAS号:
- 2109805-96-9
- 英文名:
- BAY707)
- 英文别名:
- BAY707);BAY-707
(BAY 707;BAY-707 free base;1H-Pyrrolo[2,3-b]pyridine-2-carboxamide, N-ethyl-4-[(3S)-3-methyl-4-morpholinyl]-
- 中文名:
- BAY707)
- 中文别名:
- 化合物 T14509
- CBNumber:
- CB04844527
- 分子式:
- C15H20N4O2
- 分子量:
- 288.34
- MOL File:
- 2109805-96-9.mol
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BAY707)化学性质
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密度:
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1.225±0.06 g/cm3(Predicted)
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储存条件:
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Store at -20°C
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溶解度:
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DMSO:28.83(Max Conc. mg/mL);100.0(Max Conc. mM)
Ethanol:2.88(Max Conc. mg/mL);10.0(Max Conc. mM)-
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酸度系数(pKa):
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14.36±0.40(Predicted)
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BAY707)性质、用途与生产工艺
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 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 promising in vitro pharmacokinetic 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.
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% .
BAY707)
上下游产品信息
上游原料
下游产品
2109805-96-9, BAY707) 相关搜索:
- 化合物 T14509
- 2109805-96-9
- BAY-707 free base
- 1H-Pyrrolo[2,3-b]pyridine-2-carboxamide, N-ethyl-4-[(3S)-3-methyl-4-morpholinyl]-
- BAY707)
- BAY-707
(BAY 707