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

324877
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      Overview

      Replacement Information

      Key Specifications Table

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

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      324877-5MG
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          5 mg
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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
          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

          SDS

          Title

          Safety Data Sheet (SDS) 

          Certificates of Analysis

          TitleLot Number
          324877

          References

          Reference overview
          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.