產(chǎn)品目錄

規(guī)格	10mM (in 1mL DMSO) 5mg 25mg
CAS	1303607-60-4
別名
化學(xué)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	562.50
溶解度	≥ 17.2mg/mL in DMSO
儲(chǔ)存條件	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

產(chǎn)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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1. 本產(chǎn)品僅供科研使用。請(qǐng)勿用于醫(yī)藥、臨床診斷或治療，食品及化妝品等用途。請(qǐng)勿存放于普通住宅區(qū)。

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原創(chuàng)作者：上海莼試生物技術(shù)有限公司

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