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

229103
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical FormulaCAS #
      C₂₀H₂₂N₄OS 1001478-90-5

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      229103-5MG
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          Glass bottle 5 mg
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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
          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

          SDS

          Title

          Safety Data Sheet (SDS) 

          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.