| 英文名 | 4-({[(3r,5r,6s)-1-[(1s)-2-(Tert-Butylsulfonyl)-1-Cyclopropylethyl]-6-(4-Chloro-3-Fluorophenyl)-5-(3-Chlorophenyl)-3-Methyl-2-Oxopiperidin-3-Yl]acetyl}amino)-2-Methoxybenzoic Acid |
|---|---|
| 英文别名 |
Benzoic acid, 4-[[2-[(3R,5R,6S)-6-(4-chloro-3-fluorophenyl)-5-(3-chlorophenyl)-1-[(1S)-1-cyclopropyl-2-[(1,1-dimethylethyl)sulfonyl]ethyl]-3-methyl-2-oxo-3-piperidinyl]acetyl]amino]-2-methoxy-
4-({[(3r,5r,6s)-1-[(1s)-2-(Tert-Butylsulfonyl)-1-Cyclopropylethyl]-6-(4-Chloro-3-Fluorophenyl)-5-(3-Chlorophenyl)-3-Methyl-2-Oxopiperidin-3-Yl]acetyl}amino)-2-Methoxybenzoic Acid 4-({[(3R,5R,6S)-6-(4-Chloro-3-fluorophenyl)-5-(3-chlorophenyl)-1-{(1S)-1-cyclopropyl-2-[(2-methyl-2-propanyl)sulfonyl]ethyl}-3-methyl-2-oxo-3-piperidinyl]acetyl}amino)-2-methoxybenzoic acid |
| 描述 | MDM2-p53与Kd相互作用的有效和选择性抑制剂为38 pM,IC50为1.6 nM；有效抑制肿瘤细胞系中靶细胞生长,野生型p53细胞IC50为2 nM,选择性>12,500倍超过p53缺陷细胞；表现出显着的药代动力学特性和体内抗肿瘤在SJSA-1骨肉瘤异种移植模型(ED50=2.6mg/kg QD)和HCT-116结肠直肠癌异种移植模型(ED50=10mg/kg QD)中的活性。 |
|---|---|
| 参考文献 | References 1. Rew Y, et al. J Med Chem. 2014 Dec 26;57(24):10499-511. View Related Products by Target MDM2-p53 |
| 密度 | 1.4±0.1 g/cm3 |
|---|---|
| 沸点 | 896.2±65.0 °C at 760 mmHg |
| 分子式 | C37H41Cl2FN2O7S |
| 分子量 | 747.700 |
| 闪点 | 495.8±34.3 °C |
| 精确质量 | 746.199585 |
| LogP | 7.50 |
| 蒸汽压 | 0.0±0.3 mmHg at 25°C |
| 折射率 | 1.603 |
