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324629 Eg5 Inhibitor VI - Calbiochem

324629
  
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical Formula
      C₁₃H₁₁F₃N₂O₂S
      Description
      Overview

      This product has been discontinued.



      A cell-permeable biphenylsulfamide compound that acts as a potent, reversible, and ATP-competitive inhibitor of Eg5/KSP ATPase activity (IC50 = 18 nM) with reactivity against both wild-type and the D130V mutant (Ki = 6.2 nM and 7 nM, respectively) in cell-free assays. Due to a higher ATP binding affinity of the WT enzyme, the inhibitor exhibits a much weaker antiproliferative activity against WT-expressing cells in cultures (IC50 = 5.4 and 403 nM, using HCT116 D130V and HCT116, respectively) and its in vivo antitumor efficacy has only been demonstrated in HCT116 D130V xenografed mice, but not mice with WT KSP-bearing Colo205.

      Catalogue Number324629
      Brand Family Calbiochem®
      SynonymsN-(4ʹ-(Trifluoromethyl)-4-biphenyl)sulfamide, KSP Inhibitor VI
      References
      ReferencesParrish, C.A., et al. 2007. J. Med. Chem. 50, 4939.
      Product Information
      FormOff-white solid
      Hill FormulaC₁₃H₁₁F₃N₂O₂S
      Chemical formulaC₁₃H₁₁F₃N₂O₂S
      Structure formula ImageStructure formula Image
      Applications
      Biological Information
      Purity≥97% by HPLC
      Physicochemical Information
      Dimensions
      Materials Information
      Toxicological Information
      Safety Information according to GHS
      Safety Information
      R PhraseR: 22-36/38

      Harmful if swallowed.
      Irritating to eyes and skin.
      S PhraseS: 26-36-45

      In case of contact with eyes, rinse immediately with plenty of water and seek medical advice.
      Wear suitable protective clothing.
      In case of accident or if you feel unwell, seek medical advice immediately (show the label where possible).
      Product Usage Statements
      Storage and Shipping Information
      Ship Code Ambient Temperature Only
      Toxicity Harmful
      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 6 months at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Transport Information
      Supplemental Information
      Specifications
      Global Trade Item Number
      Catalog Number GTIN
      324629 0

      Documentation

      Eg5 Inhibitor VI - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      Eg5 Inhibitor VI - Calbiochem Certificates of Analysis

      TitleLot Number
      324629

      References

      Reference overview
      Parrish, C.A., et al. 2007. J. Med. Chem. 50, 4939.
      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.

      Revision16-October-2008 JSW
      SynonymsN-(4ʹ-(Trifluoromethyl)-4-biphenyl)sulfamide, KSP Inhibitor VI
      DescriptionA cell-permeable biphenylsulfamide compound that acts as a potent, reversible, and ATP-competitive inhibitor of Eg5/KSP ATPase activity (IC50 = 18 nM) with reactivity against both wild-type and the D130V mutant (Ki = 6.2 nM and 7 nM, respectively) in cell-free assays. Due to a higher ATP binding affinity of the WT enzyme, the inhibitor exhibits a much weaker antiproliferative activity against WT-expressing cells in cultures (IC50 = 5.4 and 403 nM, using HCT116 D130V and HCT116, respectively) and its in vivo antitumor efficacy has only been demonstrated in HCT116 D130V xenografed mice, but not mice with WT KSP-bearing Colo205.
      FormOff-white solid
      Intert gas (Yes/No) Packaged under inert gas
      Chemical formulaC₁₃H₁₁F₃N₂O₂S
      Structure formulaStructure formula
      Purity≥97% by HPLC
      SolubilityDMSO (20 mg/ml) or Ethanol (15 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 6 months at -20°C.
      Toxicity Harmful
      ReferencesParrish, C.A., et al. 2007. J. Med. Chem. 50, 4939.