655203 TX-1918 - CAS 503473-32-3 - Calbiochem

655203
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical FormulaCAS #
      C₁₄H₁₂O₃ 503473-32-3

      Pricing & Availability

      Catalog Number AvailabilityPackaging Qty/Pack Price Quantity
      655203-10MG
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          Plastic ampoule 10 mg
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          Description
          OverviewA cell-permeable arylidene-cyclopentenedione derived tyrphostin that acts as a potent inhibitor for eEF2-K (IC50 = 440 nM), while it inhibits other kinases at much higher concentrations (IC50 = 4.4, 44, 44, and 440 µM for Src, PKA, PKC, and EGFR-K, respectively). Displays potent antitumor activity (EC50 = 2.07 and 230 µM in HepG2 and HCT116 tumor cells, respectively) with greatly reduced mitochondrial- (≥5000-fold) and hepato-toxicity (≥90-fold) when compared with another tyrphostin, AG 17 (Cat. No. 658425). It is therefore a more promising candidate as a therapeutic agent for cancer treatment.
          Catalogue Number655203
          Brand Family Calbiochem®
          Synonyms2-((3,5-dimethyl-4-hydroxyphenyl)-methylene)-4-cyclopentene-1,3-dione
          References
          ReferencesHori, H., et al. 2002. Bioorg. Med. Chem. 10, 3257.
          Product Information
          CAS number503473-32-3
          ATP CompetitiveN
          FormLight orange solid
          Hill FormulaC₁₄H₁₂O₃
          Chemical formulaC₁₄H₁₂O₃
          ReversibleN
          Structure formula ImageStructure formula Image
          Applications
          Biological Information
          Primary TargeteEF2-K
          Primary Target IC<sub>50</sub>440 nM against eEF2-K
          Purity≥95% by HPLC
          Physicochemical Information
          Cell permeableY
          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 Harmful
          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 1 month at -20°C.
          Packaging Information
          Packaged under inert gas Packaged under inert gas
          Transport Information
          Supplemental Information
          Specifications

          Documentation

          TX-1918 - CAS 503473-32-3 - Calbiochem SDS

          Title

          Safety Data Sheet (SDS) 

          TX-1918 - CAS 503473-32-3 - Calbiochem Certificates of Analysis

          TitleLot Number
          655203

          References

          Reference overview
          Hori, H., et al. 2002. Bioorg. Med. Chem. 10, 3257.
          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.

          Revision19-April-2011 RFH
          Synonyms2-((3,5-dimethyl-4-hydroxyphenyl)-methylene)-4-cyclopentene-1,3-dione
          DescriptionA cell-permeable arylidene-cyclopentenedione derived tyrphostin that acts as a potent inhibitor for eEF2-K (IC50 = 440 nM). Inhibits other kinases at much higher concentrations (IC50 = 4.4, 44, 44, and 440 µM for Src, PKA, PKC, and EGFR-K, respectively). Reported to exhibit potent anti-tumor activity (EC50 = 2.07 and 230 µM in HepG2 and HCT116 tumor cells, respectively) with greatly reduced mitochondrial- (≥5000-fold) and hepato-toxicity (≥90-fold) when compared with another tyrphostin, AG 17 (Cat. No. 658425). May be useful as a therapeutic agent for cancer treatment in animal models.
          FormLight orange solid
          Intert gas (Yes/No) Packaged under inert gas
          CAS number503473-32-3
          Chemical formulaC₁₄H₁₂O₃
          Structure formulaStructure formula
          Purity≥95% by HPLC
          SolubilityDMSO (10 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 1 month at -20°C.
          Toxicity Harmful
          ReferencesHori, H., et al. 2002. Bioorg. Med. Chem. 10, 3257.