Idasanutlin

SKU: orb1300933

Description

Idasanutlin (RG-7388) is a potent and selective MDM2-p53 interaction inhibitor with an IC50 of 6 nM. It is widely used in cancer research to reactivate p53 function, demonstrating efficacy in both in vitro cell-based assays and in vivo tumor models.

Research Area

Cell Biology, Protein Biochemistry

Key Properties

• CAS Number: 1229705-06-9
• MW: 616.48
• Purity: 99.86% (May vary between batches)
• Formula: C₃₁H₂₉Cl₂F₂N₃O₄
• SMILES: COc1cc(ccc1NC(=O)C1NC(CC(C)(C)C)C(C#N)(C1c1cccc(Cl)c1F)c1ccc(Cl)cc1F)C(O)=O
• Target: Mdm2|||E1/E2/E3 Enzyme
• Solubility: 20% Cremophor EL:5 mg/mL (8.11 mM);Ethanol:8 mg/mL (12.98 mM);H2O:< 1 mg/mL (insoluble or slightly soluble);DMSO:65 mg/mL (105.44 mM)

Bioactivity

• Target IC50:
  MDM2:6 nM
• In Vivo:
  In a mouse SJSA human osteosarcoma xenograft model, Idasanutlin (25 mg/kg p.o.) causes tumor growth inhibition and regression. In a SJSA xenograft model, Idasanutlin results in induction of apoptosis and antiproliferation.
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• In Vitro:
  Idasanutlin inhibits cell proliferation with IC50 of 30 nM, and induces dose-dependent p53 stabilization, cell cycle arrest, as well as cell apoptosis in cancer cells expressing wild-type p53.
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• Cell Research:
  Cell proliferation is evaluated by the tetrazolium dye assay. The concentration at which 50% inhibition (IC50) or 90% inhibition (IC90) of cell proliferation is determined from the linear regression of a plot of the logarithm of the concentration versus percent inhibition. (Only for Reference)
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

E3Enzyme, E3 ligating enzyme, E2Enzyme, E3 Enzyme, E2 Enzyme, E2 conjugating enzyme, E1 activating enzyme, E1 Enzyme, E1/E2/E3 Enzyme, E1Enzyme, inhibit, Idasanutlin, Inhibitor, Mdm2, MDM-2/p53, Ubiquitin ligase, Ubiquitin conjugating enzyme, Ubiquitin activating enzyme, Ro 5503781, RG7388, RG-7388, RG 7388

Compound Identifiers

PubChem CID

76022323