Name: MI-77301 (SAR405838)
Price: 450.00 USD

- Overview
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    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].
- Properties
  - Categories
    
    orally available MDM2 antagonist
    
    Alternative 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
    
    CAS Number
    
    1303607-60-4
    
    Molecular Formula
    
    C29H34Cl2FN3O3
    
    Molecular Weight
    
    562.50
    
    Purity
    
    98.00%
    
    Solubility
    
    ≥17.2 mg/mL in DMSO
    
    Storage
    
    Store at -20°C
    
    SMILES
    
    FC1=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
    
    * For Research Use Only