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MI-773(SAR405838)
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
MI-773(SAR405838)图片
CAS NO:1303607-60-4
包装与价格：
包装价格(元)
10mM (in 1mL DMSO)询价
5mg询价
10mg询价
50mg询价
100mg询价

MI-773 (SAR405838) (MI-77301) 是 MI-773 的类似物，是一种高效的选择性 MDM2-p53 相互作用抑制剂。 MI-773 (SAR405838) 与 MDM2 结合，Ki 为 0.88 nM。 MI-773 (SAR405838) 诱导细胞凋亡并具有有效的抗肿瘤活性。
Cas No.1303607-60-4
别名MI-77301
化学名(2'S,3R,4'S,5'R)-6-chloro-4'-(3-chloro-2-fluorophenyl)-N-((1r,4R)-4-hydroxycyclohexyl)-2'-neopentyl-2-oxospiro[indoline-3,3'-pyrrolidine]-5'-carboxamide
Canonical SMILESFC1=C(Cl)C=CC=C1[C@@H]2[C@@]3(C(C=CC(Cl)=C4)=C4NC3=O)[C@H](CC(C)(C)C)N[C@H]2C(N[C@@H]5CC[C@@H](O)CC5)=O
分子式C29H34Cl2FN3O3
分子量562.50
溶解度≥ 17.2mg/mL in DMSO
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

MI-773 (SAR405838) is a specific antagonist of MDM2 with Ki value of 0.88 nM [1].

Murine double minute 2 (MDM2) is a primary negative regulator of wild-type p53, which is a tumor suppressor. MDM2 is an E3 ubiquitin ligase that induces p53 degradation and blocks the p53 trans-activation domain (TAD) [1].

MI-773 (SAR405838) is a MDM2 antagonist. MI-773 (SAR405838) inhibited cells growth in SJSA-1, RS4;11, LNCaP and HCT-116 cancer cell lines with IC50 values of 0.092, 0.089, 0.27 and 0.20 μM, respectively. MI-773 (SAR405838) exhibited high selectivity over cancer cell lines with mutated or deleted p53 with IC50 values of >20, >10, >10 and >10 μM for HCT-116 (p53-/-), SAOS-2, PC-3 and SW620 cancer cell lines, respectively [1].

In mice bearing the SJSA-1, HCT-116, RS4;11, and LNCaP xenograft tumors, MI-773 (SAR405838) increased the levels of MDM2, p21 and p53 proteins in a dose- and time-dependent way and induced apoptosis. In the SJSA-1 xenograft model, MI-773 (SAR405838) (30-100 mg/kg) induced tumor regression and significantly inhibited tumor growth [1].

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

 
 
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