PD-166285 is a potent, ATP-competitive and broadly active protein tyrosine kinase inhibitor. It inhibits tyrosine kinases c-Src, fibroblast growth factor receptor 1 (FGFR1), and platelet-derived growth factor receptor β(PDGFRβ) (IC₅₀ values are 8.4, 39.3 and 98.3 nM respectively). PD-166285 also displays inhibitory activity against mitogen-activated protein kinase (IC₅₀ = 5 μM) and protein kinase C (IC₅₀ = 22.7 μM).