1303607-60-4

• 常用中文名：SAR405838
• 常用英文名：SAR 405838
• CAS号：1303607-60-4
• 分子式：C₂₉H₃₄Cl₂FN₃O₃
• 分子量：562.503
• 相关类别： 生物化工 抑制剂 细胞凋亡(Apoptosis) Mdm2 抑制剂
• 发布时间：2018-02-26 09:19:23
• 更新时间：2026-06-30 17:32:18
• SAR405838是一种高效的选择性MDM2抑制剂, 与MDM2结合, Ki值为0.88 nM。

名称

• 中文名: SAR405838
• 英文名: mi-77301
• 中文别名: 抑制剂(S405838); MDM2抑制剂(S405838); (2'S,3'R,4'S,5'R)-6-chloro-4'-(3-chloro-2-fluoro-phenyl)-2'-(2,2-dimethyl-propyl)-2-oxo-1,2-dihydro-spiro [indole-3,3'-pyrrolidine]-5'-cboxylic acid (trans-4-hydroxy-cyclohexyl)-amide CAS号：1303-4
• 英文别名: Spiro[3H-indole-3,3'-pyrrolidine]-5'-cboxamide, 6-chloro-4'-(3-chloro-2-fluorophenyl)-2'-(2,2-dimethylpropyl)-1,2-dihydro-N-(trans-4-hydroxycyclohexyl)-2-oxo-, (2'S,3R,4'S,5'R); Inhibitor (s405838); MI773|||MI 773|||MI-77301|||MI-773; S405838; S405838 (MI-773) //BP; S405838, 10 mM in DMSO; (2'S,3'R,4'S,5'R)-6-chloro-4'-(3-chloro-2-fluoro-phenyl)-2'-(2,2-dimethyl-propyl)-2-oxo-1,2-dihydro-spiro [indole-3,3'-pyrrolidine]-5'-carboxylic acid (trans-4-hydroxy-cyclohexyl)-amide; S405838（1303-4）; (2'S,3R,4'S,5'R)-6-chloro-4'-(3-chloro-2-fluorophenyl)-2'-(2,2-dimethylpropyl)-1,2-dihydro-N-(trans-4-hydroxycyclohexyl)-2-oxo-spiro[3H-indole-3,3'-pyrrolidine]-5'-cboxamide; S405838 (MI-773); MI-773 (2'S,3R isomer, S-405838); S405838;S-405838;S; MI-773 (S405838); MI-77301 (S405838); SAR405838; (2'S,3R,4'S,5'R)-6-Chloro-4'-(3-chloro-2-fluorophenyl)-2'-(2,2-dimethylpropyl)-N-(trans-4-hydroxycyclohexyl)-2-oxo-1,2-dihydrospiro[indole-3,3'-pyrrolidine]-5'-carboxamide; S405838, MI-77301

物化性质

• 密度: 1.4±0.1 g/cm3
• 沸点: 732.1±60.0 °C at 760 mmHg
• 分子式: C₂₉H₃₄Cl₂FN₃O₃
• 分子量: 562.503
• 闪点: 396.6±32.9 °C
• 精确质量: 561.196106
• PSA: 90.46000
• LogP: 5.79
• 外观性状: 粉末
• 蒸汽压: 0.0±2.5 mmHg at 25°C
• 折射率: 1.627
• 储存条件: -20℃

生物活性

• 描述: SAR405838是一种高效的选择性MDM2抑制剂, 与MDM2结合, Ki值为0.88 nM。
• 相关类别:
  信号通路 >> 细胞凋亡 >> MDM-2/p53
  研究领域 >> 癌症
• 参考文献:

  [1]. Wang S, et al. SAR405838: an optimized inhibitor of MDM2-p53 interaction that induces complete and durable tumor regression. Cancer Res. 2014 Oct 15;74(20):5855-5865.

  [2]. Hoffman-Luca CG, et al. Elucidation of Acquired Resistance to Bcl-2 and MDM2 Inhibitors in Acute Leukemia In Vitro and In Vivo. Clin Cancer Res. 2015 Jun 1;21(11):2558-2568.