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

229103
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Key Spec Table

Empirical FormulaCAS #
C₂₀H₂₂N₄OS1001478-90-5

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229103-5MGCN
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      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®
      SynonymsN-(3,5-dimethyl-dimethylphenyl)-2-[[5-(4-ethylphenyl)-1H-1,2,4-triazol-3-yl]sulfanyl]acetamide, CK37
      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

      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
      SynonymsN-(3,5-dimethyl-dimethylphenyl)-2-[[5-(4-ethylphenyl)-1H-1,2,4-triazol-3-yl]sulfanyl]acetamide, CK37
      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 +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 3 months at -20°c.
      Toxicity Standard Handling
      ReferencesClem, B., et al. 2011. Oncogene 30, 3370.