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首页-小分子抑制剂&激动剂-Apoptosis-MDM2-p53-Idasanutlin
Idasanutlin

Chemical Structure : Idasanutlin

CAS No.: 1229705-06-9

Idasanutlin (RG7388, RG-7388)

货号: PC-25429Not For Human Use, Lab Use Only.

Idasanutlin (RG7388) is a potent and selective p53-MDM2 inhibitor with IC50 of 6 nM in HTRF binding assays, inhibits wt-p53 cancer cell lines (SJSA1, RKO, HCT116) with mean IC50 of 0.03 uM.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Idasanutlin (RG7388) is a potent and selective p53-MDM2 inhibitor with IC50 of 6 nM in HTRF binding assays, inhibits wt-p53 cancer cell lines (SJSA1, RKO, HCT116) with mean IC50 of 0.03 uM.
Idasanutlin (RG7388) shows >300-fold selective over mutant p53 cell lines (SW480, MDA-MB435).
Idasanutlin (RG7388) effectively activated the p53 pathway in SJSA1 cells and induced tumor growth inhibition (TGI) in correlative xenografts in nude mice .
Idasanutlin (RG7388) has demonstrated the ability to activate apoptosis and induce tumor stasis with continuous treatment.

物理化学性质&存储条件

分子量 616.49
分子式 C31H29Cl2F2N3O4
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

4-((2R,3S,4R,5S)-3-(3-Chloro-2-fluorophenyl)-4-(4-chloro-2-fluorophenyl)-4-cyano-5-neopentylpyrrolidine-2-carboxamido)-3-methoxybenzoic acid

参考文献

1. Ding Q, et al. J Med Chem. 2013 Jul 25;56(14):5979-83.

2. Higgins B, et al. Clin Cancer Res. 2014 Jul 15;20(14):3742-52.

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