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229103 Choline Kinase-a Inhibitor, CK37 - CAS 1001478-90-5 - Calbiochem

Overview

Replacement Information

Key Specifications Table

CAS #Empirical Formula
1001478-90-5C₂₀H₂₂N₄OS

Products

Catalog NumberPackaging Qty/Pack
229103-5MG Glass bottle 5 mg
Description
OverviewA cell-permeable, non-Hemicholinium-3 derivative and choline-competitive choline kinase-α inhibitor. It is demonstrated to inhibit endogenous choline kinase activity, dose-dependently, between 1-10 µM, and dose-dependently decrease phosphocholine concentrations, as well as levels of downstream choline metabolites, including phosphatidylcholine and phosphatidic acid in HeLa cells. At 10 µM, it is also shown to attenuate MAPK and PI3K/AKT signaling, and disrupt the actin cytoskeleton and membrane ruffling, consistent with siRNA choline kinase-&alpha transfection. This compound exhibits dose-dependent suppression of cell growth in six tumor cell lines (IC50 = 5-10 µM), in vitro. Furthermore, it is shown to suppress tumor growth in a mouse model by 48% at 0.08 mg/g daily dose for 8 days without obvious toxicity, in vivo.
Catalogue Number229103
Brand Family Calbiochem®
SynonymsCK37, N-(3,5-dimethyl-dimethylphenyl)-2-[[5-(4-ethylphenyl)-1H-1,2,4-triazol-3-yl]sulfanyl]acetamide
References
ReferencesClem, B., et al. 2011. Oncogene 30, 3370.
Product Information
CAS number1001478-90-5
FormTan powder
Hill FormulaC₂₀H₂₂N₄OS
Chemical formulaC₂₀H₂₂N₄OS
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 3 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
229103-5MG 04055977218206

Documentation

Choline Kinase-a Inhibitor, CK37 - CAS 1001478-90-5 - Calbiochem SDS

Title

Safety Data Sheet (SDS) 

Choline Kinase-a Inhibitor, CK37 - CAS 1001478-90-5 - Calbiochem Certificates of Analysis

TitleLot Number
229103

References

Reference overview
Clem, B., et al. 2011. Oncogene 30, 3370.
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.

Revision01-May-2014 JSW
SynonymsCK37, N-(3,5-dimethyl-dimethylphenyl)-2-[[5-(4-ethylphenyl)-1H-1,2,4-triazol-3-yl]sulfanyl]acetamide
DescriptionA cell-permeable, non-Hemicholinium-3 derivative and choline-competitive choline kinase-α inhibitor. It is demonstrated to inhibit endogenous choline kinase activity, dose-dependently, between 1-10 µM, and dose-dependently decrease phosphocholine concentrations, as well as levels of downstream choline metabolites, including phosphatidylcholine and phosphatidic acid in HeLa cells. At 10 µM, it is also shown to attenuate MAPK and PI3K/AKT signaling, and disrupt the actin cytoskeleton and membrane ruffling, consistent with siRNA choline kinase-α transfection. This compound exhibits dose-dependent suppression of cell growth in six tumor cell lines (IC50 = 5-10 µM), in vitro. Furthermore, it is shown to suppress tumor growth in a mouse model by 48% at 0.08 mg/g daily dose for 8 days without obvious toxicity, in vivo.
FormTan powder
Intert gas (Yes/No) Packaged under inert gas
CAS number1001478-90-5
Chemical formulaC₂₀H₂₂N₄OS
Structure formulaStructure formula
Purity≥95% by HPLC
SolubilityDMSO (50 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 3 months at -20°c.
Toxicity Standard Handling
ReferencesClem, B., et al. 2011. Oncogene 30, 3370.