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428207 Lck Inhibitor III - CAS 1188890-30-3 - Calbiochem

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Synonyme: 2-(1H-Benzo[d]imidazol-1-yl)-N-(5-methoxy-2-methylphenyl)-6-(2-morpholinoethoxy)pyrimidin-4-amine, hydrate

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      Übersicht

      Replacement Information

      Key Spec Table

      CAS #Empirical Formula
      1188890-30-3C₂₅H₂₈N₆O₃ • H₂O
      Description
      Overview

      This product has been discontinued.



      A cell-permeable, ATP binding site-targeting, tri-substituted pyrimidine that acts as a Lck (lymphocyte specific kinase) inhibitor (IC50 = 867 nM; [ATP] = 10 µM). Shown to block IL-2 release in Jurkat E6-1 T cell line (IC50 = 1.27 µM) stimulated by CD3 cross-linking and PMA. Although less potent than Lck Inhibitor II (Cat. No. 428206), it exhibits much improved aqueous solubility (27 µg/ml in 50 mM PBS, pH 7.4, ionic strength 0.15 M) and in vivo bioavailability (F = 22%, p.o. and i.v. at 10 mg/kg).
      Catalogue Number428207
      Brand Family Calbiochem®
      Synonyms2-(1H-Benzo[d]imidazol-1-yl)-N-(5-methoxy-2-methylphenyl)-6-(2-morpholinoethoxy)pyrimidin-4-amine, hydrate
      References
      ReferencesSabat, M., et al. 2006. Bioorg. Med. Chem. Lett. 16, 5973.
      Product Information
      CAS number1188890-30-3
      FormOff-white solid
      Hill FormulaC₂₅H₂₈N₆O₃ • H₂O
      Chemical formulaC₂₅H₂₈N₆O₃ • H₂O
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Purity≥97% 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 +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
      Bestellnummer GTIN
      428207 0

      Documentation

      Lck Inhibitor III - CAS 1188890-30-3 - Calbiochem Analysenzertifikate

      TitelChargennummer
      428207

      Literatur

      Übersicht
      Sabat, M., et al. 2006. Bioorg. Med. Chem. Lett. 16, 5973.
      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.

      Revision25-May-2011 RFH
      Synonyms2-(1H-Benzo[d]imidazol-1-yl)-N-(5-methoxy-2-methylphenyl)-6-(2-morpholinoethoxy)pyrimidin-4-amine, hydrate
      DescriptionA cell-permeable, ATP binding site-targeting, tri-substituted pyrimidine that acts as a Lck (lymphocyte specific kinase) inhibitor (IC50 = 867 nM; [ATP] = 10 µM). Shown to block IL-2 release in Jurkat E6-1 T cell line (IC50 = 1.27 µM) stimulated by CD3 cross-linking and PMA. Although less potent than Lck Inhibitor II (Cat. No. 428206), it exhibits much improved aqueous solubility (27 µg/ml in 50 mM PBS, pH 7.4, ionic strength 0.15 M) and in vivo bioavailability (F = 22%, p.o. and i.v. at 10 mg/kg).
      FormOff-white solid
      Intert gas (Yes/No) Packaged under inert gas
      CAS number1188890-30-3
      Chemical formulaC₂₅H₂₈N₆O₃ • H₂O
      Structure formulaStructure formula
      Purity≥97% by HPLC
      SolubilityDMSO (100 mg/ml) or Ethanol (25 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 Regulatory Review
      ReferencesSabat, M., et al. 2006. Bioorg. Med. Chem. Lett. 16, 5973.