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    RITA (NSC 652287)
    RITA (NSC 652287)

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    This product is for research use only, not for human use. We do not sell to patients.
    数量: - + 件(库存件)
    InvivoChem Cat #: V0015
    CAS #: 213261-59-7Purity ≥98%

    Description: RITA (also known as NSC 652287) is a novel and potent inhibitor of p53-HDM-2 interaction which binds to p53dN, with a Kd of 1.5 nM, and also induces DNA-DNA cross-links. It induces both DNA-protein and DNA-DNA cross-links with no detectable DNA single-strand breaks. RITA, a drug that, like nutlin-3, can  also disrupt the p53/Mdm2 interaction. IC50: 2 nM and 20 nM for A-498 and TK-10, respectively; A series of naturally occurring and synthetic compounds containing one or more thiophene moieties have been tested in the NCI Anticancer Drug Screen and have demonstrated differential antiproliferative activity. Thiophene derivatives as a class exhibit very similar patterns of differential sensitivity, the molecular basis for which is not clear.

    Reference: Biochem Pharmacol. 1999 Jun 1;57(11):1283-95.


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    Molecular Weight (MW)292.4
    FormulaC14H12O3S2
    CAS No.213261-59-7
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 58 mg/mL (198.37 mM)
    Water:<1 mg/mL (slightly soluble or insoluble)
    Ethanol: 8 mg/mL (27.36 mM)
    Solubility (In vivo)30% Propylene glycol, 5% Tween 80, 65% D5W: 30 mg/mL
    SynonymsNSC-652287; NSC652287; NSC 652287


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    GeneralRITA is well tolerated in mice after intraperitoneal administration, with no observable weight loss at doses up to 10 mg/kg during 1 month. After five injections of 0.1 mg/kg of RITA, the growth of the HCT116 tumors is suppressed by 40%, without apparent effects on the HCT116 TP53-/- tumors. At a dose of 1 or 10 mg/kg, RITA shows strong antitumor activity.
    Animal modelSCID mice carrying HCT116 and HCT116 TP53-/- xenografts
    FormulationPhosphate buffered saline
    Dosages0.1 mg/kg, 1 mg/kg or 10 mg/kg
    Administrationi.p or i.v.
    References[1] Issaeva N, et al. Nat Med. 2004, 10(12), 1321-1328.


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

     

    RITA (NSC 652287)

     RITA (NSC 652287)


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