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    Nutlin-3a
    Nutlin-3a

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V0042
    CAS #: 675576-98-4Purity ≥98%

    Description: Nutlin-3a, the active enantiomer of Nutlin-3, is a novel and potent p53/MDM2 (murine double minute) protein protein interaction inhibitor with an IC50 of 90 nM in cell-free assays. Nutlin-3 acts by binding to MDM2 in the TP53-binding pocket, thus interfering with MDM2-directed TP53 degradation, eventually leading to the stabilization/activation of p53. Nutlin-3a has anticancer acivities . 

    References: Science. 2004 Feb 6;303(5659):844-8; Clin Cancer Res. 2009 Feb 1;15(3):933-42. 

    Related CAS: 675576-97-3 (Nutlin-3b); 890090-75-2; 548472-68-0 (Nutlin-3)

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    Molecular Weight (MW)581.49
    FormulaC30H30Cl2N4O4
    CAS No.675576-98-4
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 100 mg/mL (171.97 mM)
    Water:<1 mg/mL (slightly soluble or insoluble)
    Ethanol: N/A
    Solubility (In vivo) 5% DMSO+55% PEG 300+ddH2O: 8 mg/mL 
    Chemical Name/Synonyms4-[(4S,5R)-4,5-bis(4-chlorophenyl)-2-(4-methoxy-2-propan-2-yloxyphenyl)-4,5-dihydroimidazole-1-carbonyl]piperazin-2-one; Nutlin3a; Nutlin 3a; Nutlin-3a


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    In VitroNutlin-3a stabilizes and activates p53, and induces p21 expression in a dose-dependent manner. Nutlin-3a effectively depletes the S-phase compartment to 0.2-2% and increases the G1- and G2/M-phase compartments. Nutlin-3a induces apoptosis in ~60% of SJSA-1 and MHM cells after 40 h, which increased further after 60 h (85% and 65%, respectively)
    In VivoNutlin-3a suppresses xenograft growth in a dose-dependent fashion with the highest dose (200 mg/kg) showing a substantial tumor shrinkage. Nutlin-3 is a selective activator of the p53 pathway in vivo and highly efficacious against SJSA-1 osteosarcoma tumors
    Animal modelNude mice bearing subcutaneous human cancer xenografts
    Formulation & Dosage1% Klucel, 0.1% Tween 80; 100, 200 mg/kg; p.o.; b.i.d
    References[1] Tovar C, et al. Proc Natl Acad Sci U S A, 2006, 103(6), 1888-1893.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

    Nutlin-3a

     

    Nutlin-3a



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