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    RG-7112 (RO-5045337)
    RG-7112 (RO-5045337)

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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 #: V0045
    CAS #: 939981-39-2Purity ≥98%

    Description: RG7112 (also known as RO5045337) is a novel, potent and highly selective antagonist/inhibitor of the p53-MDM2 protein-protein interaction with IC50 of 11 nM. RG-7112 is under clinical development for cancer treatment. 

    References:  Pediatr Blood Cancer. 2013 Apr;60(4):633-41. Exp Hematol. 2014 Feb;42(2):137-45.e5.

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    Molecular Weight (MW)727.78
    FormulaC38H48Cl2N4O4S
    CAS No.939981-39-2
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 100 mg/mL (137.7 mM)
    Water:<1 mg/mL (slightly soluble or insoluble)
    Ethanol: N/A
    Solubility (In vivo)1% CMC Na:14 mg/mL
    Chemical Name[(4S,5R)-2-(4-tert-butyl-2-ethoxyphenyl)-4,5-bis(4-chlorophenyl)-4,5-dimethylimidazol-1-yl]-[4-(3-methylsulfonylpropyl)piperazin-1-yl]methanone
    SynonymRG7112; RG-7112; RG 7112; RO5045337; RO 5045337; RO5045337


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    In VitroRG7112 has been profiled extensively in many cell lines. In 15 cancer cell lines expressing wild-type p53, it shows IC50 in the range of 0.18 - 2.2 μM. However, the inhibition is much less in seven cancer cell lines with p53 mutation, IC50 5.7 - 20.3 μM. The overall selectivity is 14-fold.
    In VivoIn the SJSA1 xenograft mouse model, RG7112 (200 mg/kg, p.o.) penetrates tumor cells and activate p53 and its 2 major functions, cell-cycle arrest and apoptosis. In nude mice bearing SJSA-1, and MHMn xenografts, RG7112 (100 mg/kg, p.o.) causes tumor regression. In rats, RG7112 impairs thrombopoiesis via activation of p53.
    Animal model SJSA-1, SJSA-1luc2, and MHM xenografted Balb/c nude mice
    Formulation & Dosage 1% Klucel LF/0.1% Tween 80; 200 mg/kg; oral taken
    References[1]Pediatr Blood Cancer 2013;60:633–641


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

    RG-7112

     

    RG-7112


     

    RG-7112



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