Attention: We have moved. Merck Millipore products are no longer available for purchase on MerckMillipore.com.Learn More

219333 β-Catenin/Tcf Inhibitor IV

219333
  
Purchase on Sigma-Aldrich

Overview

Replacement Information

Key Spec Table

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 SDS

Title

Safety Data Sheet (SDS) 

β-Catenin/Tcf Inhibitor IV Certificates of Analysis

TitleLot Number
219333

References

Reference overview
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.