504045 | Focal Adhesion Kinase Inhibitor III - Calbiochem

504045
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical Formula
      C₂₂H₂₆N₄O₂S

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      5.04045.0001
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          Glass bottle 10 mg
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          Description
          OverviewA cell-permeable pyrazolobenzothiazinedioxide compound that targets and locks FAK in its inactive conformation, resulting in preincubation time-dependent inhibition in kinase assays and FAK autophosphorylation in human prostate cancer PC3M-luc cells (IC50 = 7.1 µM with 30 min inhibitor preincubation), while exhibiting little activity toward Akt1, Aurora B, HER2, MEK1, p38α, Pyk2, or Src even at concentrations as high as 10 µM.
          Catalogue Number504045
          Brand Family Calbiochem®
          SynonymsFAK Inhibitor III, N-(4-tert-Butylbenzyl)-1,5-dimethyl-1,5-dihydropyrazolo[4,3-c][2,1]benzothiazin-8-amine-4,4-dioxide
          References
          ReferencesTomita, N., et al. 2013. Bioorg. Med. Chem. Lett. 23, 1779.
          Product Information
          FormOff-white powder
          Hill FormulaC₂₂H₂₆N₄O₂S
          Chemical formulaC₂₂H₂₆N₄O₂S
          ReversibleY
          Structure formula ImageStructure formula Image
          Applications
          Biological Information
          Primary TargetFAK
          Purity≥99% by HPLC
          Physicochemical Information
          Cell permeableY
          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 -20°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

          Documentation

          SDS

          Title

          Safety Data Sheet (SDS) 

          References

          Reference overview
          Tomita, N., et al. 2013. Bioorg. Med. Chem. Lett. 23, 1779.
          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.

          Revision17-July-2013 JSW
          SynonymsFAK Inhibitor III, N-(4-tert-Butylbenzyl)-1,5-dimethyl-1,5-dihydropyrazolo[4,3-c][2,1]benzothiazin-8-amine-4,4-dioxide
          DescriptionA cell-permeable pyrazolobenzothiazinedioxide compound that targets and locks FAK in its inactive conformation, resulting in preincubation time-dependent inhibition against FAK kinase activity in cell-free assays (IC50 = 0.64 and 2.2 µM, respectively, with 60 or 5 min FAK-inhibitor preincubation before substrate poly-GT and 0.5 µM ATP addition) and FAK autophosphorylation in human prostate cancer PC3M-luc cells (IC50 = 7.1 µM with 30 min inhibitor preincubation before 2 h stimulation by plating cells on fibronectin-coated surface), while exhibiting little activity toward Akt1, Aurora B, HER2, MEK1, p38α, Pyk2, or Src even at concentrations as high as 10 µM.
          FormOff-white powder
          Intert gas (Yes/No) Packaged under inert gas
          Chemical formulaC₂₂H₂₆N₄O₂S
          Structure formulaStructure formula
          Purity≥99% by HPLC
          SolubilityDMSO (50 mg/ml)
          Storage -20°C
          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.
          Toxicity Standard Handling
          ReferencesTomita, N., et al. 2013. Bioorg. Med. Chem. Lett. 23, 1779.