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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.
      Number： - + Pieces（InventoryPieces）
      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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