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539571 InSolution™ Src Inhibitor, PP1 - Calbiochem

Overview

Replacement Information

Key Spec Table

Empirical Formula
C₁₆H₁₉N₅

Pricing & Availability

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539571-5MG
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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). 1 mg of Src Inhibitor, PP1 (Cat. No. 567809) is also available.
      Catalogue Number539571
      Brand Family Calbiochem®
      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
      FormLiquid
      FormulationA 50 mM (5 mg/355 µl) solution of Src Inhibitor, PP1 (Cat. No. 567809) in DMSO.
      Hill FormulaC₁₆H₁₉N₅
      Chemical formulaC₁₆H₁₉N₅
      Hygroscopic Hygroscopic
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Purity≥90% by HPLC
      Physicochemical Information
      Dimensions
      Materials Information
      Toxicological Information
      Safety Information according to GHS
      Safety Information
      R PhraseR: 36/38

      Irritating to eyes and skin.
      Product Usage Statements
      Storage and Shipping Information
      Ship Code Shipped with Blue Ice or with Dry Ice
      Toxicity Irritant
      Storage -20°C
      Protect from Light Protect from light
      Hygroscopic Hygroscopic
      Avoid freeze/thaw Avoid freeze/thaw
      Do not freeze Ok to freeze
      Special InstructionsFollowing initial thaw, aliquot and freeze (-20°C).
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Transport Information
      Supplemental Information
      Specifications
      Global Trade Item Number
      Catalogue Number GTIN
      539571-5MG 04055977194708

      Documentation

      InSolution™ Src Inhibitor, PP1 - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      InSolution™ Src Inhibitor, PP1 - Calbiochem Certificates of Analysis

      TitleLot Number
      539571

      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.

      Revision09-January-2012 RFH
      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).
      FormLiquid
      FormulationA 50 mM (5 mg/355 µl) solution of Src Inhibitor, PP1 (Cat. No. 567809) in DMSO.
      Intert gas (Yes/No) Packaged under inert gas
      Chemical formulaC₁₆H₁₉N₅
      Structure formulaStructure formula
      Purity≥90% by HPLC
      Storage Protect from light
      Avoid freeze/thaw
      -20°C
      Hygroscopic
      Do Not Freeze Ok to freeze
      Special InstructionsFollowing initial thaw, aliquot and freeze (-20°C).
      Toxicity Irritant
      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.