567809 | Src Inhibitor, PP1 - CAS 172889-26-8 - Calbiochem

567809
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      Overview

      Replacement Information

      Key Spec Table

      Empirical FormulaCAS #
      C₁₆H₁₉N₅172889-26-8

      Pricing & Availability

      Catalogue NumberAvailability Packaging Qty/Pack Price Quantity
      567809-1MG
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          Glass bottle 1 mg
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          Description
          OverviewA cell-permeable pyrazolopyrimidine compound that is shown to inhibit Src family tyrosine kinases Lck, Fyn, Hck, and Src (IC50 = 5, 6, 20, and 170 nM, respectively), as well as non-Src family kinases such as CSK, RIP2, and CK1δ (IC50 = 640 nM, 26 nM, 170 nM, respectively), in in vitro kinase assays. At 1 µM, in vitro kinase activity is reduced by more than 57% for p38α, p38β, CK1δ, CSK, RIP2, and GAK, while exhibiting much lower activity against more than 60 other kinases. Kinetic studies employing Src and [poly Glu-Tyr 4:1] indicate that the inhibition is mixed competitive with respect to the substrate and non-competitive with respect to ATP. PP1 also demonstrates anti-growth properties in several B lymphoma cultures of human and murine origins (IC50 = 2.5 to 8.0 µM) and pediatric brain tumor cells (IC50 = 1.1 to 9.7 µM). Also available in InSolution™ format (Cat. No. 539741).
          Catalogue Number567809
          Brand Family Calbiochem®
          Synonyms4-amino-5-(4-methylphenyl)-7-(t-butyl)pyrazolo-d-3,4-pyrimidine
          References
          ReferencesKe, J., et.al. 2009. Mol. Cancer 8, 132.
          Sikkema, A.H., et al. 2009. Cancer Res. 69, 5987.
          Bain, J., et al. 2007. Biochem. J. 408, 297.
          Bain, J., et al. 2003. Biochem. J. 371, 199.
          Karni, R., et al. 2003. FEBS Lett. 537, 47.
          Hanke, J.H., et al. 1996. J. Biol. Chem. 271, 695.
          Product Information
          CAS number172889-26-8
          FormOff-white solid
          Hill FormulaC₁₆H₁₉N₅
          Chemical formulaC₁₆H₁₉N₅
          Structure 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 Standard Handling
          Storage -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.
          Packaging Information
          Transport Information
          Supplemental Information
          Specifications

          Documentation

          SDS

          Title

          Safety Data Sheet (SDS) 

          Certificates of Analysis

          TitleLot Number
          567809

          References

          Reference overview
          Ke, J., et.al. 2009. Mol. Cancer 8, 132.
          Sikkema, A.H., et al. 2009. Cancer Res. 69, 5987.
          Bain, J., et al. 2007. Biochem. J. 408, 297.
          Bain, J., et al. 2003. Biochem. J. 371, 199.
          Karni, R., et al. 2003. FEBS Lett. 537, 47.
          Hanke, J.H., et al. 1996. J. Biol. Chem. 271, 695.
          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.

          Revision28-April-2015 JSW
          Synonyms4-amino-5-(4-methylphenyl)-7-(t-butyl)pyrazolo-d-3,4-pyrimidine
          DescriptionA cell-permeable pyrazolopyrimidine compound that is shown to inhibit Src family tyrosine kinases Lck, Fyn, Hck, and Src (IC50 = 5, 6, 20, and 170 nM, respectively), as well as non-Src family kinases such as CSK, RIP2, and CK1δ (IC50 = 640 nM, 26 nM, 170 nM, respectively), in in vitro kinase assays. At 1 µM, in vitro kinase activity is reduced by more than 57% for p38α, p38β, CK1δ, CSK, RIP2, and GAK, while exhibiting much lower activity against more than 60 other kinases. Kinetic studies employing Src and [poly Glu-Tyr 4:1] indicate that the inhibition is mixed competitive with respect to the substrate and non-competitive with respect to ATP. PP1 also demonstrates anti-growth properties in several B lymphoma cultures of human and murine origins (IC50 = 2.5 to 8.0 µM) and pediatric brain tumor cells (IC50 = 1.1 to 9.7 µM). Also available in InSolution™ format (Cat. No. 539741.
          FormOff-white solid
          CAS number172889-26-8
          Chemical formulaC₁₆H₁₉N₅
          Structure formula
          Purity≥98% by HPLC
          SolubilityDMSO (25 mg/ml)
          Storage -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 Standard Handling
          ReferencesKe, J., et.al. 2009. Mol. Cancer 8, 132.
          Sikkema, A.H., et al. 2009. Cancer Res. 69, 5987.
          Bain, J., et al. 2007. Biochem. J. 408, 297.
          Bain, J., et al. 2003. Biochem. J. 371, 199.
          Karni, R., et al. 2003. FEBS Lett. 537, 47.
          Hanke, J.H., et al. 1996. J. Biol. Chem. 271, 695.