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504045 Focal Adhesion Kinase Inhibitor III - CAS 1426683-53-5 - Calbiochem

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Synonyme: FAK Inhibitor III, N-(4-tert-Butylbenzyl)-1,5-dimethyl-1,5-dihydropyrazolo[4,3-c][2,1]benzothiazin-8-amine-4,4-dioxide

Primary Target: FAK
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504045
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Übersicht

Replacement Information

Key Spec Table

CAS #Empirical Formula
1426683-53-5C₂₂H₂₆N₄O₂S

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      		 Glasflasche 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
      CAS number1426683-53-5
      FormOff-white powder
      Hill FormulaC₂₂H₂₆N₄O₂S
      Chemical formulaC₂₂H₂₆N₄O₂S
      ReversibleY
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      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
      Global Trade Item Number
      Bestellnummer GTIN
      5.04045.0001 04055977264272

      Documentation

      Focal Adhesion Kinase Inhibitor III - CAS 1426683-53-5 - Calbiochem SDB

      Titel

      Sicherheitsdatenblatt (SDB) 

      Literatur

      Übersicht
      Tomita, N., et al. 2013. Bioorg. Med. Chem. Lett. 23, 1779.
      Datenblatt

      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
      CAS number1426683-53-5
      Chemical formulaC₂₂H₂₆N₄O₂S
      Structure formulaStructure formula
      Purity≥99% by HPLC
      SolubilityDMSO (50 mg/ml)
      Storage Protect from light
      -20°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
      ReferencesTomita, N., et al. 2013. Bioorg. Med. Chem. Lett. 23, 1779.