产品属性:
产品名称 | 规格 | CAS号 | 型号 |
MI-773 (SAR405838) | 10mM (in 1mL DMSO) 5mg 25mg | 1303607-60-4 | EY-Y0164332 |
Cas No.1303607-60-4
别名
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
分子式 C29H34Cl2FN3O3
分子量 562.5
溶解度 ≥ 17.2mg/mL in DMSO
储存条件 Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition Evaluation 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.
关键字: 1303607-60-4;C29H34Cl2FN3O3;MI-773 (SAR405838);
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