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

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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
      Quality LevelMQ100
      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.