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655200 TX-1123 - CAS 157397-06-3 - Calbiochem

A cell-permeable, reversible, and substrate-competitive arylidene-cyclopentenedione derived tyrphostin that acts as an inhibitor for Src, eEF2-K, and PKA, and EGFR-K/PKC at much higher concentrations.

TX-1123 - CAS 157397-06-3 - Calbiochem MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: 2-((3,5-di-tert-Butyl-4-hydroxyphenyl)-methylene)-4-cyclopentene-1,3-dione, PKA Inhibitor XII

Primary Target: Src
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655200
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Overview

Replacement Information

Key Spec Table

CAS #Empirical Formula
157397-06-3C₂₀H₂₄O₃

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655200-10MG
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      Description
      OverviewA cell-permeable, reversible, and substrate-competitive arylidene-cyclopentenedione derived tyrphostin that acts as an inhibitor for Src, eEF2-K, and PKA (IC50 = 2.2, 3.2, and 9.6 µM, respectively), while it inhibits EGFR-K and PKC at much higher concentrations (IC50 = 320 µM). Displays potent antitumor activity (EC50 = 3.66 and 39 µM in HepG2 and HCT116 tumor cells, respectively) with greatly reduced mitochondrial- (≥1000-fold) and hepato-toxicity (≥50-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 Number655200
      Brand Family Calbiochem®
      Synonyms2-((3,5-di-tert-Butyl-4-hydroxyphenyl)-methylene)-4-cyclopentene-1,3-dione, PKA Inhibitor XII
      References
      ReferencesHori, H., et al. 2003. Cell. Mol. Biol. Lett. 8, 528.
      Hori, H., et al. 2002. Bioorg. Med. Chem. 10, 3257.
      Product Information
      CAS number157397-06-3
      ATP CompetitiveY
      FormYellow solid
      Hill FormulaC₂₀H₂₄O₃
      Chemical formulaC₂₀H₂₄O₃
      ReversibleY
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Primary TargetSrc
      Primary Target IC<sub>50</sub>2.2, 3.2, and 9.6 µM against Src, eEF2-K, and PKA, respectively
      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 3 months at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Transport Information
      Supplemental Information
      Specifications
      Global Trade Item Number
      Catalogue Number GTIN
      655200-10MG 04055977184709

      Documentation

      TX-1123 - CAS 157397-06-3 - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      TX-1123 - CAS 157397-06-3 - Calbiochem Certificates of Analysis

      TitleLot Number
      655200

      References

      Reference overview
      Hori, H., et al. 2003. Cell. Mol. Biol. Lett. 8, 528.
      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-di-tert-Butyl-4-hydroxyphenyl)-methylene)-4-cyclopentene-1,3-dione, PKA Inhibitor XII
      DescriptionA cell-permeable, reversible and substrate-competitive arylidene-cyclopentenedione derived tyrphostin that acts as a kinase inhibitor for Src, eEF2-K, and PKA (IC50 = 2.2, 3.2, and 9.6 µM, respectively). Inhibits EGFR-K and PKC only at much higher concentrations (IC50 = 320 µM). Reported to exhibit potent anti-tumor activity (EC50 = 3.66 and 39 µM in HepG2 and HCT116 tumor cells, respectively) with greatly reduced mitochondrial- (≥1000-fold) and hepato-toxicity (≥50-fold) when compared with another tyrphostin, AG 17 (Cat. No. 658425). May be useful as a therapeutic agent for cancer treatment in animal models.
      FormYellow solid
      Intert gas (Yes/No) Packaged under inert gas
      CAS number157397-06-3
      Chemical formulaC₂₀H₂₄O₃
      Structure formulaStructure formula
      Purity≥95% by HPLC
      SolubilityDMSO (10 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 Harmful
      ReferencesHori, H., et al. 2003. Cell. Mol. Biol. Lett. 8, 528.
      Hori, H., et al. 2002. Bioorg. Med. Chem. 10, 3257.