Nutlin-3

CAS No. 548472-68-0

Nutlin-3( —— )

Catalog No. M14974 CAS No. 548472-68-0

Nutlin-3 is MDM2 antagonist. Nutlin-3 inhibits the MDM2-p53 interaction (IC50 = 0.09 μM) and activates p53.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
Size Price / USD Stock Quantity
2MG 49 In Stock
5MG 73 In Stock
10MG 113 In Stock
25MG 235 In Stock
50MG 433 In Stock
100MG 470 In Stock
200MG Get Quote In Stock
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Biological Information

  • Product Name
    Nutlin-3
  • Note
    Research use only, not for human use.
  • Brief Description
    Nutlin-3 is MDM2 antagonist. Nutlin-3 inhibits the MDM2-p53 interaction (IC50 = 0.09 μM) and activates p53.
  • Description
    Nutlin-3 is MDM2 antagonist. Nutlin-3 inhibits the MDM2-p53 interaction (IC50 = 0.09 μM) and activates p53. Antiproliferative agent;chemotherapeutic agent; induces apoptosis in Y cells.
  • In Vitro
    Nutlin-3 is an inhibitor of the MDM2-p53 interaction. In particular, co-treatment of p53-positive HCT116 cells with 1 μM of Inauhzin and 2 μM of Nutlin-3 more significantly activated p53 as measured by its protein level as well as the level of its target p21, PUMA or cleaved PARP as indication of apoptosis. Nutlin-3 is a small-molecule inhibitor that acts to inhibit MDM2 binding to p53 and subsequent p53-dependent DNA damage signaling. As a single agent, Nutlin-3 (2-10 μM) stabilizes p53 and p21WAF levels and is toxic to WTp53-22RV1 cells (IC50, 4.3 μM) but has minimal toxicity toward p53-deficient cells (IC50, >10 μM). Nutlin-3 induces p53 and p21WAF expression in a dose-dependent manner in 22RV1 cells. Short-term cell cycle assays show that, at a dose of 10 μM, Nutlin-3 increasea slightly the G1-phase fraction and decreasea S-phase fraction of all three cell lines.
  • In Vivo
    Nutlin-3 can suppress the growth of xenograft tumors derived from human osteosarcoma or leukemia cells, the anti-tumor activity of Nutlin-3 even at the dose of 200 mg/kg per oral administration is marginal in an HCT116-derived xenograft tumor model. Nutlin-3 may be a useful adjunct to improve the therapeutic ratio using precision radiotherapy targeted to hypoxic cells and warrants further study in vivo.
  • Synonyms
    ——
  • Pathway
    Apoptosis
  • Target
    MDM2-p53
  • Recptor
    p53-MDM2
  • Research Area
    Cancer
  • Indication
    ——

Chemical Information

  • CAS Number
    548472-68-0
  • Formula Weight
    581.49
  • Molecular Formula
    C30H30Cl2N4O4
  • Purity
    >98% (HPLC)
  • Solubility
    DMSO: 10 mM
  • SMILES
    COC1=CC(OC(C)C)=C(C=C1)C1=NC(C(N1C(=O)N1CCNC(=O)C1)C1=CC=C(Cl)C=C1)C1=CC=C(Cl)C=C1
  • Chemical Name
    ——

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1.Stéphane Supiot, et al. Molecular Y Therapeutics (2008), 7(4), 993-999.
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