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

575547
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Overview

Replacement Information

Key Spec Table

CAS #Empirical Formula
664993-53-7C₂₅H₂₆N₂O₅

Products

Catalogue NumberPackaging Qty/Pack
575547-25MG Glass bottle 25 mg
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®
SynonymsN-(4-((4-(4-Methoxyphenyl)tetrahydro-2H-pyran-4-yl)methylcarbamoyl)phenyl)furan-2-carboxamide, TNKS1/2 Inhibitor IV, Wnt Pathway Inhibitor XVII
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
Catalogue Number GTIN
575547-25MG 04055977265903

Documentation

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

Title

Safety Data Sheet (SDS) 

Tankyrase1/2 Inhibitor IV, JW55 - CAS 664993-53-7 - Calbiochem Certificates of Analysis

TitleLot Number
575547

References

Reference overview
Waaler, J., et al. 2012. Cancer Res. 72, 2822.
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.

Revision11-October-2013 JSW
SynonymsN-(4-((4-(4-Methoxyphenyl)tetrahydro-2H-pyran-4-yl)methylcarbamoyl)phenyl)furan-2-carboxamide, TNKS1/2 Inhibitor IV, Wnt Pathway Inhibitor XVII
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.