AG 1879
4-Amino-5-(4-chlorophenyl)-7-(t-butyl)pyrazolo[3,4-d]pyrimidine Off-white solid. PACKAGED UNDER INERT GAS. A potent 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). Purity: ≥95% by HPLC. Ref.: 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. |
