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    InvivoChem Cat #: V0040
    CAS #: 890090-75-2Purity ≥98%

    Description: Nutlin-3, a tetra-substituted imidazoline, is a novel potent and selective small-molecule antagonist/inhibitor of murine double minute 2 (MDM2) with potential antitumor activities. Nutlin-3 is essentially a PPI (protein protein interaction) inhibitor, it acts by occupying the binding site of p53 in MDM2 and consequently preventing MDM2 binding to p53, which leads to the disruption of the autoregulator feedback loop and the fostering of the p53 tumor suppressor network. It also binds to murine double minute 4 (MDM4), which is another component of the p35 tumor surveillance pathway. Nutlin-3 binds MDM2 in the TP53-binding pocket, thereby interfering with MDM2-directed TP53 degradation. isrupts its interaction with p53, leading to the stabilization and activation of p53.

    References: Science. 2004 Feb 6;303(5659):844-8; Nature. 2006 Nov 2;444(7115):61-6.

    Related CAS:548472-68-0 (Nutlin-3); 675576-98-4 (Nutlin-3a); 675576-97-3 (Nutlin-3b)

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    Molecular Weight (MW)581.5
    CAS No.890090-75-2
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 100 mg/mL (171.9 mM)
    Water:<1 mg/mL (slightly soluble or insoluble)
    Ethanol: 30 mg/mL (51.59 mM)
    Solubility (In vivo)O=C(N1C(C2=C(C=C(C=C2)OC)OC(C)C)=N[[email protected]](C3=CC=C(C=C3)Cl)[[email protected]@H]1C4=CC=C(C=C4)Cl)N5CC(NCC5)=O.
    Chemical Name/Synonyms4-[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-3 treatment induces the expression of MDM2 and p21, and displays potent antiproliferative activity with IC50 of ~1.5 μM, only in cells with wild-type p53 such as HCT116, RKO and SJSA-1, but not in the mutant p53 cell lines SW480 and MDA-MB-435.
    In VivoOral administration of Nutlin-3 at 200 mg/kg twice daily for 3 weeks significantly inhibits the tumor growth of SJAS-1 xenografts by 90%, comparable with the effect of doxorubicin treatment with 81% inhibition of tumor growth.
    Animal modelAthymic female nude mice (Nu/Nu-nuBR) injected subcutaneously with SJSA-1 cells
    Formulation & DosageFormulated in 2% Klucel, 0.5% Tween 80; 100 mg/kg; Oral BID
    References[1] Vassilev LT, et al. Science, 2004, 303(5659), 844-848.

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







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