219331 β-Catenin/Tcf Inhibitor II, PKF118-310 - Calbiochem

Overview

Replacement Information

Key Specifications Table

Empirical Formula
C₇H₇N₅O₂

Pricing & Availability

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219331-10MG
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      Glass bottle 10 mg
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      Description
      OverviewA synthetic cell-permeable actinobacteria pyrimidotriazine-dione that selectively disrupts β-catenin-Tcf4 interaction (IC50 = 0.8 µM in cell-free binding assays) and inhibits β-catenin-regulated cellular transcription activity (IC50 = 0.3 µM in HCT116-based reporter assays). PKF118-310 is demonstrated to reverse β-catenin, but not siamois, mRNA-induced ventral body axis formation in Xenopus embryos, while direct tumor site injection (1 mg/kg/0.5 wk) in HepG2 xenograph mice is shown to increase the number of apoptotic cells and decrease the expression of β-catenin target genes (cyclin D1, c-Myc, survivin) in the tumor mass, resulting in an effective tumor growth retardation (by ~60% after a 4-wk treatment period) in vivo.
      Catalogue Number219331
      Brand Family Calbiochem®
      Synonyms1,6-Dimethylpyrimido[5,6-e][1,2,4]triazine-5,7-dione, Wnt Pathway Inhibitor X
      References
      ReferencesWei, W., et al. 2010. Int. J. Cancer 126, 2426.
      Lepourcelet, M., et al. 2004. Cancer Cell 5, 91.
      Product Information
      FormDark yellow solid
      Hill FormulaC₇H₇N₅O₂
      Chemical formulaC₇H₇N₅O₂
      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 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

      Documentation

      β-Catenin/Tcf Inhibitor II, PKF118-310 - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      β-Catenin/Tcf Inhibitor II, PKF118-310 - Calbiochem Certificates of Analysis

      TitleLot Number
      219331

      References

      Reference overview
      Wei, W., et al. 2010. Int. J. Cancer 126, 2426.
      Lepourcelet, M., et al. 2004. Cancer Cell 5, 91.
      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.

      Revision03-April-2012 JSW
      Synonyms1,6-Dimethylpyrimido[5,6-e][1,2,4]triazine-5,7-dione, Wnt Pathway Inhibitor X
      DescriptionA synthetic cell-permeable actinobacteria pyrimidotriazine-dione that selectively disrupts β-catenin-Tcf4 interaction (IC50 = 0.8 µM in cell-free binding assays) and inhibits β-catenin-regulated cellular transcription activity (IC50 = 0.3 µM in HCT116-based reporter assays). PKF118-310 is demonstrated to reverse β-catenin, but not siamois, mRNA-induced ventral body axis formation in Xenopus embryos, while direct tumor site injection (1 mg/kg/0.5 wk) in HepG2 xenograph mice is shown to increase the number of apoptotic cells and decrease the expression of β-catenin target genes (cyclin D1, c-Myc, survivin) in the tumor mass, resulting in an effective tumor growth retardation (by ~60% after a 4-wk treatment period) in vivo.
      FormDark yellow solid
      Intert gas (Yes/No) Packaged under inert gas
      Chemical formulaC₇H₇N₅O₂
      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
      ReferencesWei, W., et al. 2010. Int. J. Cancer 126, 2426.
      Lepourcelet, M., et al. 2004. Cancer Cell 5, 91.