Overview

  • Product name
    MI-773, MDM2 inhibitor
  • Description
    Highly potent, selective MDM2 inhibitor
  • Alternative names
    • MI 77301
    • SAR405838
  • Biological description

    A spiro-oxindole that acts as a highly potent, selective MDM2 inhibitor. Binds to MDM2 (Ki = 0.88 nM) and blocks the MDM2-p53 interaction. Activates wild-type p53 in vitro and in xenograft tumor tissue of leukemia and solid tumors, leading to p53-dependent cell cycle arrest and/or apoptosis.

  • Purity
    > 98%
  • CAS Number
    1303607-60-4
  • Chemical structure
    Chemical Structure

Properties

  • 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
  • Molecular weight
    562.51
  • Molecular formula
    C29H34Cl2FN3O3
  • PubChem identifier
    53476877
  • Storage instructions
    Shipped at 4°C. Store at -20°C. Store under desiccating conditions.
  • Solubility overview
    Soluble in DMSO to 100 mM
  • Handling

    Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour.

    Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details.

  • SMILES
    CC(C)(C)C[C@H]1[C@@]2([C@H]([C@@H](N1)C(=O)NC3CCC(CC3)O)C4=C(C(=CC=C4)Cl)F)C5=C(C=C(C=C5)Cl)NC2=O
  • Source

    Synthetic

References

This product has been referenced in:
  • Zhao Y  et al. Small-molecule inhibitors of the MDM2-p53 protein-protein interaction (MDM2 Inhibitors) in clinical trials for cancer treatment. J Med Chem 58:1038-52 (2015). Read more (PubMed: 25396320) »
  • Hoffman-Luca CG  et al. Elucidation of Acquired Resistance to Bcl-2 and MDM2 Inhibitors in Acute Leukemia In Vitro and In Vivo. Clin Cancer Res 21:2558-68 (2015). Read more (PubMed: 25754349) »
  • Wang S  et al. SAR405838: an optimized inhibitor of MDM2-p53 interaction that induces complete and durable tumor regression. Cancer Res 74:5855-65 (2014). Read more (PubMed: 25145672) »

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Please note: All products are "FOR RESEARCH USE ONLY AND ARE NOT INTENDED FOR DIAGNOSTIC OR THERAPEUTIC USE, NOT FOR USE IN HUMANS"

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