529573 PP2 - CAS 172889-27-9 - Calbiochem

529573
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical FormulaCAS #
      C₁₅H₁₆ClN₅ 172889-27-9

      Pricing & Availability

      Catalog Number AvailabilityPackaging Qty/Pack Price Quantity
      529573-1MG
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          Plastic ampoule 1 mg
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          529573-5MG
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              Glass bottle 5 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
              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 SDS

              Title

              Safety Data Sheet (SDS) 

              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.


              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.