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553015 Raf Kinase Inhibitor V - CAS 918505-84-7 - Calbiochem

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      Aperçu

      Replacement Information

      Tableau de caractéristiques principal

      CAS #Empirical Formula
      918505-84-7C₁₇H₁₄ClF₂N₃O₃S
      Description
      OverviewA cell-permeable azaindole compound that interacts with Raf via both the ATP-binding site and a "Raf-selective pocket" that exhibits conformation-dependent inhibitor-binding modes and accounts for the compound's preferential binding and inhibitory activity toward the active Raf mutants (IC50 = 6.7, 13, 130, 160, and >1,300 nM against C-Raf-1Y340D/Y341D, B-RafV600E, BRK, WT B-Raf, and 64 other kinases, respectively). Shown to inhibit the proliferation and cellular Erk phosphorylation much more potently in B-RafV600E-bearing than WT B-Raf-bearing cancer cell lines in vitro and effectively suppress COLO205-derived tumor growth in mice in vivo (near complete regression during the 1-wk treatment period; 20 mg/kg, daily, p.o.).
      Catalogue Number553015
      Brand Family Calbiochem®
      SynonymsPropane-1-sulfonic acid-(3-(5-chloro-1H-pyrrolo[2,3-b]pyridine-3-carbonyl)-2,4-difluoro-phenyl)-amide, PLX4720
      References
      ReferencesTsai, J., et al. 2008. Proc. Natl. Acad. Sci. USA 105, 3041.
      Product Information
      CAS number918505-84-7
      FormOrange-yellow solid
      Hill FormulaC₁₇H₁₄ClF₂N₃O₃S
      Chemical formulaC₁₇H₁₄ClF₂N₃O₃S
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Purity≥95% by HPLC
      Physicochemical Information
      Dimensions
      Materials Information
      Toxicological Information
      Safety Information according to GHS
      Safety Information
      Product Usage Statements
      Storage and Shipping Information
      Ship Code Ambient Temperature Only
      Toxicity Standard Handling
      Storage +2°C to +8°C
      Protect from Light Protect from light
      Do not freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Transport Information
      Supplemental Information
      Specifications
      Global Trade Item Number
      Référence GTIN
      553015 0

      Documentation

      Raf Kinase Inhibitor V - CAS 918505-84-7 - Calbiochem FDS

      Titre

      Fiche de données de sécurité des matériaux (FDS) 

      Raf Kinase Inhibitor V - CAS 918505-84-7 - Calbiochem Certificats d'analyse

      TitreNuméro de lot
      553015

      Références bibliographiques

      Aperçu de la référence bibliographique
      Tsai, J., et al. 2008. Proc. Natl. Acad. Sci. USA 105, 3041.
      Fiche technique

      Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

      Revision25-May-2011 RFH
      SynonymsPropane-1-sulfonic acid-(3-(5-chloro-1H-pyrrolo[2,3-b]pyridine-3-carbonyl)-2,4-difluoro-phenyl)-amide, PLX4720
      DescriptionA cell-permeable azaindole compound that interacts with Raf via both the ATP-binding site and a "Raf-selective pocket" that exhibits conformation-dependent inhibitor-binding modes and accounts for the compound's preferential binding and inhibitory activity toward the active Raf mutants (IC50 = 6.7, 13, 130, 160, and >1,300 nM against C-Raf-1Y340D/Y341D, B-RafV600E, BRK, WT B-Raf, and 64 other kinases, respectively). Shown to inhibit the proliferation and cellular Erk phosphorylation much more potently in B-RafV600E-bearing than WT B-Raf-bearing cancer cell lines in vitro and effectively suppress COLO205-derived tumor growth in mice in vivo (near complete regression during the 1-wk treatment period; 20 mg/kg, daily p.o.).
      FormOrange-yellow solid
      Intert gas (Yes/No) Packaged under inert gas
      CAS number918505-84-7
      Chemical formulaC₁₇H₁₄ClF₂N₃O₃S
      Structure formulaStructure formula
      Purity≥95% by HPLC
      SolubilityDMSO (100 mg/ml) or Ethanol (5 mg/ml)
      Storage Protect from light
      +2°C to +8°C
      Do Not Freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
      Toxicity Standard Handling
      ReferencesTsai, J., et al. 2008. Proc. Natl. Acad. Sci. USA 105, 3041.