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

203661
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical FormulaCAS #
      C₂₅H₂₄N₆O₂ 936563-87-0

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      203661-1MG
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          Glass bottle 1 mg
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          Description
          OverviewA 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
          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

          Documentation

          SDS

          Title

          Safety Data Sheet (SDS) 

          Certificates of Analysis

          TitleLot Number
          203661

          References

          Reference overview
          Pan, Z., et al. 2007. ChemMedchem. 2, 58.
          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-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 -20°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 3 months at -20°C.
          Toxicity Regulatory Review
          ReferencesPan, Z., et al. 2007. ChemMedchem. 2, 58.