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575547 Tankyrase1/2 Inhibitor IV, JW55 - CAS 664993-53-7 - Calbiochem

The Tankyrase1/2 Inhibitor IV, JW55 controls the biological activity of Tankyrase1/2. This small molecule/inhibitor is primarily used for Biochemicals applications.

FDS (Fiches de données de sécurité), certificats d’analyse (CoA) et de qualité (CoQ), dossiers, brochures et autres documents disponibles.

Synonymes: TNKS1/2 Inhibitor IV, Wnt Pathway Inhibitor XVII, N-(4-((4-(4-Methoxyphenyl)tetrahydro-2H-pyran-4-yl)methylcarbamoyl)phenyl)furan-2-carboxamide

Primary Target: tankyrase 1 and 2
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575547
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Tableau de caractéristiques principal

CAS #Empirical Formula
664993-53-7C₂₅H₂₆N₂O₅

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575547-25MG
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      Description
      OverviewA cell-permeable phenylcarbamoylfuran-carboxamide compound that acts as a potent, selective, and reversible inhibitor of poly(ADP-ribosyl)ation activity of tankyrase 1 and 2 (IC50 = 1.9 and 0.83 µM, respectively). Exhibits high selectivity over PARP1 (IC50 = 20 µM). Stabilizes and increases AXIN2 levels, thereby enhancing phosphorylation and degradation of β-catenin resulting in reduced canonical Wnt signaling (IC50 = 470 nM in Wnt 3a-induced HEK293 cells transfected with ST-Luc). Shown to induce cell cycle arrest and diminish the proliferation of SW480 colorectal cancer cells (~ 5 µM). Suppresses tumor growth in tamoxifen-induced polyposis in Apc knock-out murine model (100 mg/kg, i.p.). Displays adequate human liver microsomal stability (t1/2 = 10.1 min).
      Catalogue Number575547
      Brand Family Calbiochem®
      SynonymsTNKS1/2 Inhibitor IV, Wnt Pathway Inhibitor XVII, N-(4-((4-(4-Methoxyphenyl)tetrahydro-2H-pyran-4-yl)methylcarbamoyl)phenyl)furan-2-carboxamide
      References
      ReferencesWaaler, J., et al. 2012. Cancer Res. 72, 2822.
      Product Information
      CAS number664993-53-7
      FormOff-white solid
      Hill FormulaC₂₅H₂₆N₂O₅
      ReversibleY
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Primary Target tankyrase 1 and 2
      Purity≥99% 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 +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
      Référence GTIN
      575547-25MG 04055977265903

      Documentation

      Tankyrase1/2 Inhibitor IV, JW55 - CAS 664993-53-7 - Calbiochem FDS

      Titre

      Fiche de données de sécurité des matériaux (FDS) 

      Tankyrase1/2 Inhibitor IV, JW55 - CAS 664993-53-7 - Calbiochem Certificats d'analyse

      TitreNuméro de lot
      575547

      Références bibliographiques

      Aperçu de la référence bibliographique
      Waaler, J., et al. 2012. Cancer Res. 72, 2822.
      Fiche technique

      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.

      Revision11-October-2013 JSW
      SynonymsTNKS1/2 Inhibitor IV, Wnt Pathway Inhibitor XVII, N-(4-((4-(4-Methoxyphenyl)tetrahydro-2H-pyran-4-yl)methylcarbamoyl)phenyl)furan-2-carboxamide
      DescriptionA cell-permeable phenylcarbamoylfuran-carboxamide compound that acts as a potent, selective, and reversible inhibitor of poly(ADP-ribosyl)ation activity of tankyrase 1 and 2 (IC50 = 1.9 and 0.83 µM, respectively). Exhibits high selectivity over PARP1 (IC50 = 20 µM). Stabilizes and increases AXIN2 levels, thereby enhancing phosphorylation and degradation of β-catenin resulting in reduced canonical Wnt signaling (IC50 = 470 nM in Wnt 3a-induced HEK293 cells transfected with ST-Luc). Shown to induce cell cycle arrest and diminish the proliferation of SW480 colorectal cancer cells (~ 5 µM). Suppresses tumor growth in tamoxifen-induced polyposis in Apc knock-out murine model (100 mg/kg, i.p.). Displays adequate human liver microsomal stability (t1/2 = 10.1 min).
      FormOff-white solid
      Intert gas (Yes/No) Packaged under inert gas
      CAS number664993-53-7
      Structure formulaStructure formula
      Purity≥99% HPLC
      SolubilityDMSO (100 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 Standard Handling
      ReferencesWaaler, J., et al. 2012. Cancer Res. 72, 2822.