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A cell-permeable, potent inhibitor of Tcf4-luciferase expression in both 33.13 and 22C11 cells (IC₅₀ = 596, 690 nM, respectively). Arrests the growth of colon cancer cells.
More>>A cell-permeable, potent inhibitor of Tcf4-luciferase expression in both 33.13 and 22C11 cells (IC₅₀ = 596, 690 nM, respectively). Arrests the growth of colon cancer cells. Less<<
β-Catenin/Tcf Inhibitor IV MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.
A 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 Number
219333
Brand Family
Calbiochem®
Synonyms
6-Chloro-N-(4-(((2-(methylamino)quinazolin-4-yl)amino)methyl)phenyl)nicotinamide, Wnt Pathway Inhibitor XVIII
References
References
Dehnhardt, C.M., et al. 2010. J. Med. Chem.53, 897.
Product Information
Form
Off-white solid
Hill Formula
C₂₂H₁₉ClN₆O
Chemical formula
C₂₂H₁₉ClN₆O
Structure formula Image
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 Instructions
Following 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
产品目录编号
GTIN
219333-5MGCN
04055977202120
Documentation
β-Catenin/Tcf Inhibitor IV 分析证书
标题
批号
219333
参考
参考信息概述
Dehnhardt, C.M., et al. 2010. J. Med. Chem.53, 897.
数据表
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.
Revision
21-March-2014 JSW
Synonyms
6-Chloro-N-(4-(((2-(methylamino)quinazolin-4-yl)amino)methyl)phenyl)nicotinamide, Wnt Pathway Inhibitor XVIII
Description
A 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.
Form
Off-white solid
Intert gas (Yes/No)
Packaged under inert gas
Chemical formula
C₂₂H₁₉ClN₆O
Structure formula
Purity
≥95% by HPLC
Solubility
DMSO (100 mg/ml)
Storage
Protect from light
+2°C to +8°C
Do Not Freeze
Ok to freeze
Special Instructions
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Toxicity
Standard Handling
References
Dehnhardt, C.M., et al. 2010. J. Med. Chem.53, 897.
