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

567809
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Empirical FormulaCAS #
C₁₆H₁₉N₅ 172889-26-8

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567809-1MG
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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 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 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

      Src Inhibitor, PP1 - CAS 172889-26-8 - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      Src Inhibitor, PP1 - CAS 172889-26-8 - Calbiochem 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 formulaStructure 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.