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

428207
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical FormulaCAS #
      C₂₅H₂₈N₆O₃ • H₂O 1188890-30-3

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      428207-5MG
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          Plastic ampoule 5 mg
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          Description
          OverviewA 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
          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

          Documentation

          SDS

          Title

          Safety Data Sheet (SDS) 

          Certificates of Analysis

          TitleLot Number
          428207

          References

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

          Brochure

          Title
          Biologics 35.1
          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.

          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 +2°C to +8°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
          ReferencesSabat, M., et al. 2006. Bioorg. Med. Chem. Lett. 16, 5973.