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MI-77301 (SAR405838)

Catalog No.
B4984
orally available MDM2 antagonist
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$250.00
Ship with 10-15 days
5mg
$138.00
Ship with 10-15 days
25mg
$558.00
Ship with 10-15 days

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

Background

MI-77301 (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-77301 (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-77301 (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-77301 (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-77301 (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.

Chemical Properties

StorageStore at -20°C
M.Wt562.50
Cas No.1303607-60-4
Formula C29H34Cl2FN3O3
Solubility≥17.2 mg/mL in DMSO
Chemical Name(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
SDFDownload SDF
Canonical SMILESFC1=C(Cl)C=CC=C1[[email protected]@H]2[[email protected]@]3(C(C=CC(Cl)=C4)=C4NC3=O)[[email protected]](CC(C)(C)C)N[[email protected]]2C(N[[email protected]@H]5CC[[email protected]@H](O)CC5)=O
Shipping ConditionEvaluation sample solution: ship with blue ice. All other available sizes: ship with RT, or blue ice upon request.
General tipsFor obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while. Stock solution can be stored below -20°C for several months.

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