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    Vemurafenib (PLX4032; RG7204; RO5185426)
    Vemurafenib (PLX4032; RG7204; RO5185426)

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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 #: V1001
    CAS #: 918504-65-1Purity ≥98%

    Description: Vemurafenib (formerly PLX-4032; RG7204; RG-7204; RO5185426; RO-5185426; PLX4032; trade name: Zelboraf) is a potent and selective inhibitor of B-RafV600E mutated form with potential antineoplastic activity. It inhibits B-RafV600E with an IC50 of 31 nM in enzymatic assay. As an orally bioavailable, ATP-competitive and small-molecule inhibitor of BRAF(V600E) kinase, vemurafenib was approved by FDA  in 2011 for the treatment of late-stage melanoma. Vemurafenib selectively binds to the ATP-binding site of BRAF(V600E) kinase and inhibits its activity, which may result in an inhibition of an over-activated MAPK signaling pathway downstream in BRAF(V600E) kinase-expressing tumor cells and a reduction in tumor cell proliferation.

    References: Yang H, et al. Cancer Res, 2010, 70(13), 5518-5527.

    Related CAS #: 918504-65-1; 918505-61-0 (analog); 

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    Molecular Weight (MW)489.92
    FormulaC23H18ClF2N3O3S
    CAS No.918504-65-1; 918505-61-0 (vemurafenib analog) 
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 97 mg/mL (198.0 mM)
    Water: <1 mg/mL (slightly soluble or insoluble)
    Ethanol: <1 mg/mL
    Solubility (In vivo)4% DMSO+30% PEG 300+5% Tween 80+ddH2O: 5 mg/mL
    Synonym

    Vemurafenib; RO5185426; RG7204; PLX 4032; RG 7204; RO 5185426; RG-7204; RO5185426; PLX4032; PLX-4032; trade name: Zelboraf

    Chemical Name: N-(3-(5-(4-chlorophenyl)-1H-pyrrolo[2,3-b]pyridine-3-carbonyl)-2,4-difluorophenyl)propane-1-sulfonamide


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    GeneralABT-199 (100 mg/kg) causes a maximal tumor growth inhibition of 95% and tumor growth delay of 152% in RS4;11 xenografts.
    Animal modelMice (athymic nude) xenograft models of LOX, Colo829, and A375 cells
    FormulationFormulated as microprecipitated bulk powder (MBP), suspended at the desired concentration in an aqueous vehicle containing 2% Klucel LF, and adjusted to pH 4 with dilute HCl
    Dosages12.5 mg/kg–100 mg/kg
    AdministrationOral gavage twice a day
    Reference[1] Yang H, et al. Cancer Res, 2010, 70(13), 5518-5527.


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

    Vemurafenib (PLX4032, RG7204)

    Mol Cancer Ther; 15(8); 1859–69, 2016

    Vemurafenib (PLX4032, RG7204)Vemurafenib (PLX4032, RG7204)


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