529573 PP2 - CAS 172889-27-9 - Calbiochem

529573
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Replacement Information

Key Spec Table

Empirical FormulaCAS #
C₁₅H₁₆ClN₅172889-27-9

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529573-1MGCN
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      Plastic ampoule 1 mg
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      Description
      OverviewA potent, reversible, ATP-competitive, and selective inhibitor of the Src family of protein tyrosine kinases. Inhibits p56lck (IC50 = 4 nM), p59fynT (IC50 = 5 nM), Hck (IC50 = 5 nM), and Src (IC50 = 100 nM). Does not significantly affect the activity of EGFR kinase (IC50 = 480 nM), JAK2 (IC50 > 50 µM), or ZAP-70 (IC50 >100 µM). Inhibits the activation of focal adhesion kinase and its phosphorylation at Tyr577. Also potently inhibits anti-CD3-stimulated tyrosine phosphorylation of human T cells (IC50 = 600 nM). A 10 mM (1 mg/331 µl) solution of PP2 (Cat. No. 529576) in DMSO also available.
      Catalogue Number529573
      Brand Family Calbiochem®
      SynonymsAG 1879, 4-Amino-5-(4-chlorophenyl)-7-(t-butyl)pyrazolo[3,4-d]pyrimidine
      References
      ReferencesKarni, R., et al. 2003. FEBS Lett. 537, 47.
      Salazar, E.P., and Rozengurt, E. 1999. J. Biol. Chem. 274, 28371.
      Hanke, J.H., et al. 1996. J. Biol. Chem. 271, 695.



      Selected Citations
      Lee, J., et al. 2009. Cell Stem Cell 5, 76.


      Product Information
      CAS number172889-27-9
      ATP CompetitiveY
      FormOff-white solid
      Hill FormulaC₁₅H₁₆ClN₅
      Chemical formulaC₁₅H₁₆ClN₅
      ReversibleY
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Primary Target p56lck
      Primary Target IC<sub>50</sub>4 nM, 5 nM, 5 nM, 100 nM, against p56lck, p59fynT, Hck, and Src, respectively; 600 nM against anti-CD3-stimulated tyrosine phosphorylation of human T cells
      Purity≥95% by HPLC
      Physicochemical Information
      Cell permeableN
      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, refrigerate (4°C). Stock solutions are stable for up to 6 months at 4°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Transport Information
      Supplemental Information
      Specifications

      Documentation

      PP2 - CAS 172889-27-9 - Calbiochem Certificates of Analysis

      TitleLot Number
      529573

      References

      Reference overview
      Karni, R., et al. 2003. FEBS Lett. 537, 47.
      Salazar, E.P., and Rozengurt, E. 1999. J. Biol. Chem. 274, 28371.
      Hanke, J.H., et al. 1996. J. Biol. Chem. 271, 695.



      Selected Citations
      Lee, J., et al. 2009. Cell Stem Cell 5, 76.


      Brochure

      Title
      Bulk Product Guide

      Technical Info

      Title
      JAK/STAT Signaling Research Focus

      Citations

      Title
    • Dance, M., et al. 2006. Journal of Biological Chemistry 281, 23285.
    • Fukumoto, S., et al. 2006. Journal of Biological Chemistry 281, 5008.
    • Heiss, E., et al. 2006. Blood 108, 1542.
    • Jafri, F., et al. 2006. Journal of Biological Chemistry 281, 19346.
    • Olivera, A., et al. 2006. Journal of Biological Chemistry 281, 2515.
    • Rayala, S.K. et al. 2006. Journal of Biological Chemistry 281, 4395.
    • Ellen J. Tisdale and Cristina R. Artalejo. 2006. Journal of Biological Chemistry 281, 8436.
    • Meyn, M.A., et al. 2005. Molecular Pharmacology 68, 1320.
    • Summy, J.M., et al. 2005. Molecular Cancer Therapeutics 4, 1900.
    • Trevino, J.G., et al. 2005. Cancer Research 65, 7214.
    • Liao, X., et al. 2003. Endocrinology 144, 1656.
    • Cross, M.J., et al. 2002. Molecular Biology of the Cell 13, 2881.
    • 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.

      Revision12-January-2010 RFH
      SynonymsAG 1879, 4-Amino-5-(4-chlorophenyl)-7-(t-butyl)pyrazolo[3,4-d]pyrimidine
      DescriptionA potent, reversible, ATP-competitive, and selective inhibitor of the src family of tyrosine kinases that is similar to PP1. Selectively inhibits p56lck (IC50 = 4 nM), p59fynT (IC50 = 5 nM), Hck (IC50 = 5 nM), and Src (IC50 = 100 nM) compared to other tyrosine kinases, such as EGF-R (IC50 = 480 nM), JAK2 (IC50 >50 µM) or ZAP-70 (IC50 >100 µM). Also potently inhibits anti-CD3-stimulated tyrosine phosphorylation of human T cells (IC50 = 600 nM).
      FormOff-white solid
      Intert gas (Yes/No) Packaged under inert gas
      CAS number172889-27-9
      Chemical formulaC₁₅H₁₆ClN₅
      Structure formulaStructure formula
      Purity≥95% by HPLC
      SolubilityDMSO (20 mg/ml). Further dilute with aqueous buffers just prior to use.
      Storage -20°C
      Do Not Freeze Ok to freeze
      Special InstructionsFollowing reconstitution, refrigerate (4°C). Stock solutions are stable for up to 6 months at 4°C.
      Toxicity Standard Handling
      ReferencesKarni, R., et al. 2003. FEBS Lett. 537, 47.
      Salazar, E.P., and Rozengurt, E. 1999. J. Biol. Chem. 274, 28371.
      Hanke, J.H., et al. 1996. J. Biol. Chem. 271, 695.



      Selected Citations
      Lee, J., et al. 2009. Cell Stem Cell 5, 76.


      Citation
    • Dance, M., et al. 2006. Journal of Biological Chemistry 281, 23285.
    • Fukumoto, S., et al. 2006. Journal of Biological Chemistry 281, 5008.
    • Heiss, E., et al. 2006. Blood 108, 1542.
    • Jafri, F., et al. 2006. Journal of Biological Chemistry 281, 19346.
    • Olivera, A., et al. 2006. Journal of Biological Chemistry 281, 2515.
    • Rayala, S.K. et al. 2006. Journal of Biological Chemistry 281, 4395.
    • Ellen J. Tisdale and Cristina R. Artalejo. 2006. Journal of Biological Chemistry 281, 8436.
    • Meyn, M.A., et al. 2005. Molecular Pharmacology 68, 1320.
    • Summy, J.M., et al. 2005. Molecular Cancer Therapeutics 4, 1900.
    • Trevino, J.G., et al. 2005. Cancer Research 65, 7214.
    • Liao, X., et al. 2003. Endocrinology 144, 1656.
    • Cross, M.J., et al. 2002. Molecular Biology of the Cell 13, 2881.