219333 β-Catenin/Tcf Inhibitor IV

219333
  
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      Áttekintés

      Replacement Information

      Kulcsspecifikációk táblázata

      Empirical Formula
      C₂₂H₁₉ClN₆O
      Description
      OverviewA cell-permeable diaminoquinazoline compound that potently inhibits Tcf4-luciferase expression in both 33.13 and 22C11 cells and only minimally affects 5A8 control cells (IC50 = 596, 690 and > 2984 nM, respectively), and arrests the growth of 33.13, HT29, DLD1 and LoVo colon cancer cells (IC50 = 648, 1375, 1739 and 1400 nM, respectively). Displays moderate solubility (23 µg/ml at pH 7.4) and microsomal stability in rat (t1/2 = 17 mins), exerts preferential antiproliferative effect towards activated β-catenin signaling over K-ras in a RK3E differential adherent assay (K-ras/β-Cat ~ 2.8) and suppresses the in vivo growth of a β-catenin/RK3E tumor xenograft in nude mice (19 mg/kg, i.p.). Shown to alter the gene expression levels of several cyclins, phosphatases and transcription factors and overlap with the siRNA knockdown of β-catenin or Tcf4 profile in HT29 cells.
      Catalogue Number219333
      Brand Family Calbiochem®
      Synonyms6-Chloro-N-(4-(((2-(methylamino)quinazolin-4-yl)amino)methyl)phenyl)nicotinamide, Wnt Pathway Inhibitor XVIII
      References
      ReferencesDehnhardt, C.M., et al. 2010. J. Med. Chem. 53, 897.
      Product Information
      FormOff-white solid
      Hill FormulaC₂₂H₁₉ClN₆O
      Chemical formulaC₂₂H₁₉ClN₆O
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Purity≥95% by HPLC
      Physicochemical Information
      Dimensions
      Materials Information
      Toxicological Information
      Safety Information according to GHS
      Safety Information
      Product Usage Statements
      Storage and Shipping Information
      Ship Code Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
      Toxicity Standard Handling
      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

      Documentation

      β-Catenin/Tcf Inhibitor IV MSDS

      Title

      Safety Data Sheet (SDS) 

      β-Catenin/Tcf Inhibitor IV Certificates of Analysis

      TitleLot Number
      219333

      References

      Hivatkozások áttekintése
      Dehnhardt, C.M., et al. 2010. J. Med. Chem. 53, 897.
      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.

      Revision21-March-2014 JSW
      Synonyms6-Chloro-N-(4-(((2-(methylamino)quinazolin-4-yl)amino)methyl)phenyl)nicotinamide, Wnt Pathway Inhibitor XVIII
      DescriptionA cell-permeable diaminoquinazoline compound that potently inhibits Tcf4-luciferase expression in both 33.13 and 22C11 cells and only minimally affects 5A8 control cells (IC50 = 596, 690 and > 2984 nM, respectively), and arrests the growth of 33.13, HT29, DLD1 and LoVo colon cancer cells (IC50 = 648, 1375, 1739 and 1400 nM, respectively). Displays moderate solubility (23 µg/ml at pH 7.4) and microsomal stability in rat (t1/2 = 17 mins), exerts preferential antiproliferative effect towards activated β-catenin signaling over K-ras in a RK3E differential adherent assay (K-ras/β-Cat ~ 2.8) and suppresses the in vivo growth of a β-catenin/RK3E tumor xenograft in nude mice (19 mg/kg, i.p.). Shown to alter the gene expression levels of several cyclins, phosphatases and transcription factors and overlap with the siRNA knockdown of β-catenin or Tcf4 profile in HT29 cells.
      FormOff-white solid
      Intert gas (Yes/No) Packaged under inert gas
      Chemical formulaC₂₂H₁₉ClN₆O
      Structure formulaStructure formula
      Purity≥95% by HPLC
      SolubilityDMSO (100 mg/ml)
      Storage +2°C to +8°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 6 months at -20°C.
      Toxicity Standard Handling
      ReferencesDehnhardt, C.M., et al. 2010. J. Med. Chem. 53, 897.