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    PLX-4720
    PLX-4720

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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 #: V1002
    CAS #: 918505-84-7Purity ≥98%

    Description: PLX4720 (PLX-4720; PLX 4720), a 7-azaindole/pyrrolopyridine-based vemurafenib derivative discovered by a structure-guided discovery approach, is a novel, potent and selective inhibitor of B-RafV600E mutant with potential antitumor activity. It inhibits B-RafV600E with an IC50 of 13 nM in a cell-free assay, and is 10-fold more selective for B-RafV600E over wild-type B-Raf. PLX-4720 potently inhibits ERK phosphorylation in tumor cell lines harboring B-RafV600E, induces cell cycle arrest and apoptosis in B-RafV600E-positive melanoma cells and causes tumor growth delays in B-RafV600E-dependent tumor xenograft models through oral administration.

    References: Proc Natl Acad Sci U S A. 2008 Feb 26;105(8):3041-6.

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    Molecular Weight (MW)413.83
    FormulaC17H14ClF2N3O3S
    CAS No.918505-84-7
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 83 mg/mL (200.6 mM)
    Water: <1 mg/mL (slightly soluble or insoluble)
    Ethanol: <1 mg/mL
    Solubility (In vivo)2% DMSO+50% PEG 300+5% Tween 80+ddH2O: 5 mg/mL
    Other info
    Synonym: PLX 4720; PLX4720; PLX-4720.
    IUPAC/Chemical Name: N-(3-(5-chloro-1H-pyrrolo[2,3-b]pyridine-3-carbonyl)-2,4-difluorophenyl)propane-1-sulfonamide
    InChi Key: YZDJQTHVDDOVHR-UHFFFAOYSA-N
    InChi Code: InChI=1S/C17H14ClF2N3O3S/c1-2-5-27(25,26)23-13-4-3-12(19)14(15(13)20)16(24)11-8-22-17-10(11)6-9(18)7-21-17/h3-4,6-8,23H,2,5H2,1H3,(H,21,22)
    SMILES Code: CCCS(=O)(NC1=CC=C(F)C(C(C2=CNC3=NC=C(Cl)C=C32)=O)=C1F)=O 


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    GeneralOral administration of PLX-4720 at 20 mg/kg/day induces significant tumor growth delays and regressions in B-RafV600E-dependent COLO205 tumor xenografts, without obvious adverse effects in mice even at dose of 1 g/kg.
    Animal modelFemale athymic mice (NCr nu/nu) implanted s.c. with COLO205 cells, and SCID mice with 1205Lu or C8161 cells
    Formulation Suspended in vehicle (5% DMSO, 1% methylcellulose)
    Dosages5, 20, or 100 mg/kg
    AdministrationAdministered orally once or twice daily
    Reference[1] Tsai J, et al. Proc Natl Acad Sci U S A, 2008, 105(8), 3041-3046.


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

    PLX-4720

    Antimetastatic effects of PLX4720 require NK cells. Cancer Res; 74(24); 7298–308, 2014

    PLX-4720

    PLX4720 requires perforin and CD226 for optimal antimetastatic activity.

    PLX-4720

    qPCR analysis showing that PLX4720 (3μM) alters the expression of XBP1s mRNA.


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