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203661 Bruton's Tyrosine Kinase Inhibitor III - CAS 936563-87-0 - Calbiochem

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Synonyme: 1-(3-(4-Amino-3-(4-phenyloxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-en-1-one, N-Acryloyl-(3-(4-Amino-3-(4-phenyloxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidine

203661
  
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      Übersicht

      Replacement Information

      Key Spec Table

      CAS #Empirical Formula
      936563-87-0C₂₅H₂₄N₆O₂
      Description
      Overview

      This product has been discontinued.



      A cell-permeable pyrrolopyridinyl-acryloyl compound that acts as a highly potent, selective, and irreversible inhibitor of BTK (IC50 = 720 pM), while affecting Lyn, Lck, and Itk activity only at much higher concentrations (IC50 = 14 nM, 97 nM, and 1.0 µM, respectively). Inhibits BTK-dependent PLC-γ1 phosphorylation and Ca2+ flux in human B cell line Ramos in vitro (IC50 = 14 nM and 40 nM, respectively) and is of excellent efficacy in a murine rheumatoid archritis model in vivo (>95% inhibition at 10 mg/kg/day, p.o.).
      Catalogue Number203661
      Brand Family Calbiochem®
      Synonyms1-(3-(4-Amino-3-(4-phenyloxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-en-1-one, N-Acryloyl-(3-(4-Amino-3-(4-phenyloxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidine
      References
      ReferencesPan, Z., et al. 2007. ChemMedchem. 2, 58.
      Product Information
      CAS number936563-87-0
      FormWhite crystalline solid
      Hill FormulaC₂₅H₂₄N₆O₂
      Chemical formulaC₂₅H₂₄N₆O₂
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Purity≥98% by HPLC
      Physicochemical Information
      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 Regulatory Review
      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
      Bestellnummer GTIN
      203661 0

      Documentation

      Bruton's Tyrosine Kinase Inhibitor III - CAS 936563-87-0 - Calbiochem Analysenzertifikate

      TitelChargennummer
      203661

      Literatur

      Übersicht
      Pan, Z., et al. 2007. ChemMedchem. 2, 58.
      Datenblatt

      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-May-2011 RFH
      Synonyms1-(3-(4-Amino-3-(4-phenyloxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-en-1-one, N-Acryloyl-(3-(4-Amino-3-(4-phenyloxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidine
      DescriptionA cell-permeable pyrrolopyridinyl-acryloyl compound that acts as a highly potent, selective, and irreversible inhibitor of BTK (IC50 = 720 pM), while affecting Lyn, Lck, and Itk activity only at much higher concentrations (IC50 = 14 nM, 97 nM, and 1.0 µM, respectively). Inhibits BTK-dependent PLC-γ1 phosphorylation and Ca2+ flux in human B cell line Ramos in vitro (IC50 = 14 nM and 40 nM, respectively) and is of excellent efficacy in a murine rheumatoid archritis model in vivo (>95% inhibition at 10 mg/kg/day, p.o.).
      FormWhite crystalline solid
      Intert gas (Yes/No) Packaged under inert gas
      CAS number936563-87-0
      Chemical formulaC₂₅H₂₄N₆O₂
      Structure formulaStructure formula
      Purity≥98% by HPLC
      SolubilityDMSO (10 mg/ml) or Ethanol (5 mg/ml). Fresh DMSO is recommended.
      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 Regulatory Review
      ReferencesPan, Z., et al. 2007. ChemMedchem. 2, 58.