Overview

  • Product name

    RG-7112, MDM2 inhibitor
  • Description

    Potent, orally bioavailable MDM2 inhibitor
  • Alternative names

    • RO5045337
  • Biological description

    Potent, orally bioavailable MDM2 inhibitor that displays antineoplastic activity. Nutlin imidazoline compound. RG-7112 binds to MDM2, thereby preventing the binding of the MDM2 protein to the transcriptional activation domain of the tumor suppressor protein p53. Binds MDM2 with KD = 10.7 nM. Blocks the p53- MDM2 interaction with an IC50 of 18 nM in HTRF assays.

  • Purity

    > 98%
  • CAS Number

    939981-39-2
  • Chemical structure

    Chemical Structure

Properties

  • Chemical name

    ((4S,5R)-2-(4-(tert-butyl)-2-ethoxyphenyl)-4,5-bis(4-chlorophenyl)-4,5-dimethyl-4,5-dihydro-1H-imidazol-1-yl)(4-(3-(methylsulfonyl)propyl)piperazin-1-yl)methanone 

  • Molecular weight

    727.78
  • Molecular formula

    C38H48Cl2N4O4S
  • PubChem identifier

    57406853
  • Storage instructions

    Shipped at Room Temperature. Store at -20°C. It is important to note that this is air sensitive and impurities can occur as a result of air oxidation. Store In the Dark. Store under desiccating conditions.
  • Solubility overview

    DMSO 100 mg/mL (138 mM)

    Ethanol 100 mg/mL (138 mM)

    Insoluble in water

     

  • 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

    CCOC1=C(C=CC(=C1)C(C)(C)C)C2=NC(C(N2C(=O)N3CCN(CC3)CCCS(=O)(=O)C)(C)C4=CC=C(C=C4)Cl)(C)C5=CC=C(C=C5)Cl
  • Source

    Synthetic

References

This product has been referenced in:

  • Zhang Z  et al. Discovery of potent and selective spiroindolinone MDM2 inhibitor, RO8994, for cancer therapy. Bioorg Med Chem 22:4001-9 (2014). Read more (PubMed: 24997575) »
  • Tovar C  et al. MDM2 small-molecule antagonist RG7112 activates p53 signaling and regresses human tumors in preclinical cancer models. Cancer Res 73:2587-97 (2013). Read more (PubMed: 23400593) »
  • Vu B  et al. Discovery of RG7112: A Small-Molecule MDM2 Inhibitor in Clinical Development. ACS Med Chem Lett 4:466-9 (2013). Read more (PubMed: 24900694) »

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Please note: All products are "FOR RESEARCH USE ONLY. NOT FOR USE IN DIAGNOSTIC PROCEDURES, NOT FOR USE IN HUMANS"
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