SAR405838

• 常用名: SAR405838
• 英文名: SAR 405838
• CAS号: 1303607-60-4
• 分子量: 562.503
• 密度: 1.4±0.1 g/cm3
• 沸点: 732.1±60.0 °C at 760 mmHg
• 分子式: C₂₉H₃₄Cl₂FN₃O₃
• 熔点: N/A
• 闪点: 396.6±32.9 °C

SAR405838用途

SAR405838是一种高效的选择性MDM2抑制剂, 与MDM2结合, Ki值为0.88 nM。

SAR405838名称

• 中文名: SAR405838
• 英文名: mi-77301

SAR405838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.

SAR405838物理化学性质

• 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
• InChIKey: IDKAKZRYYDCJDU-AEPXTFJPSA-N
• SMILES: CC(C)(C)CC1NC(C(=O)NC2CCC(O)CC2)C(c2cccc(Cl)c2F)C12C(=O)Nc1cc(Cl)ccc12
• 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℃

SAR405838靶点实验

查看更多实验

实验名称：In vivo induction of cleaved PARP upregulation in human SJSA1 cell tumor xenografted ... 来源：ChEMBL 靶标：Mus musculus External Id：CHEMBL4011396

实验名称：In vivo induction of cleaved caspase-3 upregulation in human SJSA1 cell tumor xenogra... 来源：ChEMBL 靶标：Mus musculus External Id：CHEMBL4011397

实验名称：Oral bioavailability in rat at 25 mg/kg 来源：ChEMBL 靶标：Rattus norvegicus External Id：CHEMBL4011394

实验名称：In vivo induction of p53 activation in human SJSA1 cell tumor xenografted in SCID mou... 来源：ChEMBL 靶标：Mus musculus External Id：CHEMBL4011395

实验名称：Cytotoxicity against human SJSA1 cells assessed as growth inhibition after 16 hrs by ... 来源：ChEMBL 靶标：SJSA-1 External Id：CHEMBL3241173

实验名称：Inhibition of MDM4 (14 to 111 residues)/p53 (unknown origin) interaction expressed in... 来源：ChEMBL 靶标：Protein Mdm4 External Id：CHEMBL5378738

实验名称：Half life in rat at 25 mg/kg, po 来源：ChEMBL 靶标：Rattus norvegicus External Id：CHEMBL4011390

实验名称：Antitumor activity against human SJSA1 cells xenografted in mouse assessed as tumor r... 来源：ChEMBL 靶标：SJSA-1 External Id：CHEMBL3413431

实验名称：Inhibition of MDM2 (1 to 118 residues)/p53 (unknown origin) interaction expressed in ... 来源：ChEMBL 靶标：E3 ubiquitin-protein ligase Mdm2 External Id：CHEMBL5378737

实验名称：Antitumor activity against human LNCAP cells xenografted in mouse assessed as tumor r... 来源：ChEMBL 靶标：LNCaP External Id：CHEMBL3413430

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SAR405838英文别名

• (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
• (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
• SAR405838
• SAR 405838