324877 Focal Adhesion Kinase Inhibitor I - CAS 4506-66-5 - Calbiochem

324877
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Empirical FormulaCAS #
C₆H₁₀N₄ • 4HCl 4506-66-5

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      Description
      OverviewA cell-permeable tetraamine compound that is identified from a computer-aided molecular docking screening based on Fak Y397 interaction and is shown to inhibit FAK (Cat. No. 324876) autophosphorylation as well as its kinase activity toward paxillin phosphorylation both in cell-free kinase assays (IC50 <1 µM) and in BT474 breast cancer cultures, while exhibiting little activity against Pyk2 (Cat. No. 662067) autophosphorylation or the kinase activity of c-Raf, c-Src, EGFR, VEGFR-3, IGF-1, Met, PDGFR-α, Pyk2, and PI 3-K (p110δ/p85α). Reported to inhibit BT474 proliferation both in cultures in vitro (IC50 ~10 µM) and in mice in vivo (~25% of no treatment controls on day 23; 30 mg/kg via 5 i.p/wk).
      Catalogue Number324877
      Brand Family Calbiochem®
      SynonymsFAK Inhibitor I, 1,2,4,5-Benzenetetraamine, 4HCl, NSC 667249
      References
      ReferencesGolubovskaya, V.M., et al. 2008. J. Med. Chem. 51, 7405.
      Product Information
      CAS number4506-66-5
      FormGrey solid
      Hill FormulaC₆H₁₀N₄ • 4HCl
      Chemical formulaC₆H₁₀N₄ • 4HCl
      Hygroscopic Hygroscopic
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Purity≥95% by elemental analysis
      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
      Hygroscopic Hygroscopic
      Do not freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Transport Information
      Supplemental Information
      Specifications

      Documentation

      Focal Adhesion Kinase Inhibitor I - CAS 4506-66-5 - Calbiochem MSDS

      Title

      Safety Data Sheet (SDS) 

      Focal Adhesion Kinase Inhibitor I - CAS 4506-66-5 - Calbiochem Certificates of Analysis

      TitleLot Number
      324877

      References

      Przegląd literatury
      Golubovskaya, V.M., et al. 2008. J. Med. Chem. 51, 7405.
      Data Sheet

      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.

      Revision03-June-2010 RFH
      SynonymsFAK Inhibitor I, 1,2,4,5-Benzenetetraamine, 4HCl, NSC 667249
      DescriptionA cell-permeable tetraamine compound that is identified from a computer-aided molecular docking screening based on Fak Y397 interaction and is shown to inhibit FAK (Cat. No. 324876) autophosphorylation as well as its kinase activity toward paxillin phosphorylation both in cell-free kinase assays (IC50 <1 µM) and in BT474 breast cancer cultures, while exhibiting little activity against Pyk2 (Cat. No. 662067) autophosphorylation or the kinase activity of c-Raf, c-Src, EGFR, VEGFR-3, IGF-1, Met, PDGFR-α, Pyk2, and PI 3-K (p110δ/p85α). Reported to inhibit BT474 proliferation both in cultures in vitro (IC50 ~10 µM) and in mice in vivo (~25% of no treatment controls on day 23; 30 mg/kg via 5 i.p/wk).
      FormGrey solid
      Intert gas (Yes/No) Packaged under inert gas
      CAS number4506-66-5
      Chemical formulaC₆H₁₀N₄ • 4HCl
      Structure formulaStructure formula
      Purity≥95% by elemental analysis
      SolubilityH₂O (14 mg/ml) or DMSO (50 mg/ml)
      Storage +2°C to +8°C
      Hygroscopic
      Protect from light
      Do Not Freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
      Toxicity Standard Handling
      ReferencesGolubovskaya, V.M., et al. 2008. J. Med. Chem. 51, 7405.