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343021 Flt-3 Inhibitor II - CAS 896138-40-2 - Calbiochem

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

Synonymes: Bis-(5-hydroxy-1H-indol-2-yl)methanone, PDGFR Tyrosine Kinase Inhibitor XI

Primary Target: Flt-3
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343021
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Tableau de caractéristiques principal

CAS #Empirical Formula
896138-40-2C₁₇H₁₂N₂O₃

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      Description
      Overview

      This product has been discontinued.



      A cell-permeable symmetrical indolylmethanone kinase inhibitor that is more selective toward Flt3 over PDGFR either in cell-based receptor autophosphorylation (IC50 = 40 nM vs. 300 nM) or in cell-free kinase reactions (IC50 = 33 nM vs. 171 nM) and potently induces apoptosis in Flt3-expressing primary AML patient blasts. Affects Abl- or Kit-dependent cell growth only at much higher concentrations (IC50 = 4.2 and ≥0.5 µM, respectively), while exhibiting little effect against IL-3-mediated cellular signaling. The molecular mechanism of inhibition is presumably due to interaction at the enzyme's ATP-binding site.
      Catalogue Number343021
      Brand Family Calbiochem®
      SynonymsBis-(5-hydroxy-1H-indol-2-yl)methanone, PDGFR Tyrosine Kinase Inhibitor XI
      References
      ReferencesMahboobi, S., et al. 2006. J. Med. Chem. 49, 3101.
      Product Information
      CAS number896138-40-2
      ATP CompetitiveN
      FormYellowish brown solid
      Hill FormulaC₁₇H₁₂N₂O₃
      Chemical formulaC₁₇H₁₂N₂O₃
      ReversibleN
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Primary TargetFlt-3
      Primary Target IC<sub>50</sub>40 nM against Flt3 in cell-based receptor autophosphorylation; 33 nM against Flt3 in cell-free kinase reactions
      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 Irritant
      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 3 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
      343021-1MG 04055977195026

      Documentation

      Flt-3 Inhibitor II - CAS 896138-40-2 - Calbiochem Certificats d'analyse

      TitreNuméro de lot
      343021

      Références bibliographiques

      Aperçu de la référence bibliographique
      Mahboobi, S., et al. 2006. J. Med. Chem. 49, 3101.
      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.

      Revision14-September-2007 JSW
      SynonymsBis-(5-hydroxy-1H-indol-2-yl)methanone, PDGFR Tyrosine Kinase Inhibitor XI
      DescriptionA cell-permeable symmetrical indolylmethanone kinase inhibitor that is more selective toward Flt3 over PDGFR either in cell-based receptor autophosphorylation (IC50 = 40 nM vs. 300 nM) or in cell-free kinase reactions (IC50 = 33 nM vs. 171 nM) and potently induces apoptosis in Flt3-expressing primary AML patient blasts. Affects Abl- or Kit-dependent cell growth only at much higher concentrations (IC50 = 4.2 and ≥0.5 µM, respectively), while exhibiting little effect against IL-3-mediated cellular signaling. The molecular mechanism of inhibition is presumably due to interaction at the enzyme's ATP-binding site.
      FormYellowish brown solid
      Intert gas (Yes/No) Packaged under inert gas
      CAS number896138-40-2
      Chemical formulaC₁₇H₁₂N₂O₃
      Structure formulaStructure formula
      Purity≥95% by HPLC
      SolubilityDMSO (100 mg/ml) or Ethanol (5 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 3 months at -20°C.
      Toxicity Irritant
      ReferencesMahboobi, S., et al. 2006. J. Med. Chem. 49, 3101.