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402081 Indirubin Derivative E804 - CAS 854171-35-0 - Calbiochem

FDS (Fiches de données de sécurité), certificats d’analyse (CoA) et de qualité (CoQ), dossiers, brochures et autres documents disponibles.

Synonymes: IDR E804

Primary Target: Src
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      Aperçu

      Replacement Information

      Tableau de caractéristiques principal

      CAS #Empirical Formula
      854171-35-0C₂₀H₁₉N₃O₄
      Description
      Overview

      This product has been discontinued.



      A cell-permeable indirubin derivative (IDR) that blocks the Src-Stat3 signaling pathway and displays anti-tumor properties. Shown to be a potent, reversible, and ATP-competitive inhibitor of the kinase activities of Src (IC50 = 430 nM), Cdk1/cyclin E (IC50 = 210 nM), Cdk2/cyclin A (IC50 = 540 nM), and Cdk1/cyclin B (IC50 = 1.65 µM). Reduces the tyrosine phosphorylation levels of Src, JAK1, and Stat3 in MDA-MB-468 cells in a time- and dose-dependent manner. Selectively induces apoptosis in cells expressing high levels of active Stat3, but not cells lacking activated Stat3. The apoptotic effect of E804 is shown to be due to the down-regulation of antiapoptotic proteins Mcl-1 and survivin.
      Catalogue Number402081
      Brand Family Calbiochem®
      SynonymsIDR E804
      References
      ReferencesNam, S., et al. 2005. Proc. Natl. Acad. Sci. USA 102, 5998.
      Product Information
      CAS number854171-35-0
      ATP CompetitiveY
      FormDark red solid
      Hill FormulaC₂₀H₁₉N₃O₄
      Chemical formulaC₂₀H₁₉N₃O₄
      ReversibleY
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Primary TargetSrc
      Primary Target IC<sub>50</sub>430 nM, 210 nM, 540 nM, 1.65 µM, against Src, Cdk1/cyclin E, Cdk2/cyclin A, and Cdk1/cyclin B, 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 Shipped with Blue Ice or with Dry Ice
      Toxicity Standard Handling
      Storage -20°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 6 months at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Transport Information
      Supplemental Information
      Specifications
      Global Trade Item Number
      Référence GTIN
      402081 0

      Documentation

      Indirubin Derivative E804 - CAS 854171-35-0 - Calbiochem FDS

      Titre

      Fiche de données de sécurité des matériaux (FDS) 

      Références bibliographiques

      Aperçu de la référence bibliographique
      Nam, S., et al. 2005. Proc. Natl. Acad. Sci. USA 102, 5998.

      Brochure

      Titre
      An Introduction to Inhibitors and Their Biological Applications - 1st Edition

      Informations techniques

      Titre
      JAK/STAT Signaling Research Focus
      Fiche technique

      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.

      Revision13-April-2011 RFH
      SynonymsIDR E804
      DescriptionA cell-permeable indirubin derivative (IDR) that blocks the Src-Stat3 signaling pathway and displays anti-tumor properties. Shown to be a potent, reversible, and ATP-competitive inhibitor of the kinase activities of Src (IC50 = 430 nM), Cdk1/cyclin E (IC50 = 210 nM), Cdk2/cyclin A (IC50 = 540 nM), and Cdk1/cyclin B (IC50 = 1.65 µM). Reduces the tyrosine phosphorylation levels of Src, JAK1, and Stat3 in MDA-MB-468 cells in a time- and dose-dependent manner. Selectively induces apoptosis in cells expressing high levels of active Stat3, but not cells lacking activated Stat3. The apoptotic effect of E804 is shown to be due to the down-regulation of antiapoptotic proteins Mcl-1 and survivin.
      FormDark red solid
      Intert gas (Yes/No) Packaged under inert gas
      CAS number854171-35-0
      Chemical formulaC₂₀H₁₉N₃O₄
      Structure formulaStructure formula
      Purity≥95% by HPLC
      SolubilityDMSO (200 mg/ml)
      Storage Protect from light
      -20°C
      Do Not Freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
      Toxicity Standard Handling
      ReferencesNam, S., et al. 2005. Proc. Natl. Acad. Sci. USA 102, 5998.