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PLX-4720

Cat. No.:YN350213

  • CAS No. :918505-84-7

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    • 产品名称: PLX-4720
      CAS No.: 918505-84-7
      Chemical Name: N-[3-[(5-chloro-1H-pyrrolo[2,3-b]pyridin-3-yl)carbonyl]-2,4-difluorophenyl]-1-propanesulfonamide
      Synonyms:PLX4720
      分子量:413.83
      分子式:C₁₇H₁₄ClF₂N₃O₃S
      SMILES:O=S(NC1=CC=C(C(C(C2=CNC3=NC=C(C=C23)Cl)=O)=C1F)F)(CCC)=O
      存储:Please store the product under the recommended conditions in theCertificate of Analysis.
      运输:Room temperature in continental US; may vary elsewhere.
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      Purity: 98%
    • 产品描述: PLX-4720 是一种有效的,选择性的B-RafV600E抑制剂,IC50值为 13 nM;与对 c-Raf-1 的选择性相同,是野生型 B-Raf 选择性的 10 倍。
      IC50和靶点: [{name:"B-RafV600E:13 nM (IC50)"},{name: "B-Raf:160 nM (IC50)"},{name: "BRK:130 nM (IC50)"},{name: "FRK:1300 nM (IC50)"},{name: "Csk:1500 nM (IC50)"},{name: "Src:1700 nM (IC50)"},{name: "FAK:1700 nM (IC50)"},{name: "FGFR:1900 nM (IC50)"},{name: "KDR:2300 nM (IC50)"},{name: "HGK:2800 nM (IC50)"},{name: "CSF1R:3300 nM (IC50)"},{name: "Aurora A:3400 nM (IC50)"}]
      In Vitro:
      In Vivo:
      Clinical Trial:
      Solvent & Solubility:
    • Lyons, J.F., Wilhelm, S., Hibner, B., et al.Discovery of a novel Raf kinase inhibitorEndocr. Relat. Cancer8(3),219-225(2001)

      Wang, X., and Kim, J.Conformation-specific effects of Raf kinase inhibitorsJ. Med. Chem.55(17),7332-7341(2012)

      Flaherty, K.T., Puzanov, I., Kim, K.B., et al.Inhibition of mutated, activated BRAF in metastatic melanomaN. Engl. J. Med.363(9),809-819(2010)

      Old, W.M., Shabb, J.B., Houel, S., et al.Functional proteomics identifies targets of phosphorylation by B-Raf signaling in melanomaMol. Cell34(1),115-131(2009)

      Nucera, C., Porrello, A., Antonello, Z.A., et al.B-RafV600E and thrombospondin-1 promote thyroid cancer progressionProc. Natl. Acad. Sci. USA107(23),10649-10654(2010)

      Tsai, J., Lee, J.T., Wang, W., et al.Discovery of a selective inhibitor of oncogenic B-Raf kinase with potent antimelanoma activityProc. Natl. Acad. Sci. USA105(8),3041-3046(2008)

      Nucera, C., Nehs, M.A., Nagarkatti, S.S., et al.Targeting BRAFV600E with PLX4720 displays potent antimigratory and anti-invasive activity in preclinical models of human thyroid cancerOncologist16(3),296-309(2011)

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