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

The β-Catenin/Tcf Inhibitor II, PKF118-310 controls the biological activity of β-Catenin/Tcf. This small molecule/inhibitor is primarily used for Cancer applications.

MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: 1,6-Dimethylpyrimido[5,6-e][1,2,4]triazine-5,7-dione, Wnt Pathway Inhibitor X

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219331
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Overview

Replacement Information

Key Specifications Table

Empirical Formula
C₇H₇N₅O₂

Products

Catalog NumberPackaging Qty/Pack
219331-10MG Glass bottle 10 mg
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
Global Trade Item Number
Catalog Number GTIN
219331-10MG 04055977202106

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