PD158780 is a highly potent, selective, ATP binding site inhibitor of EGFR with IC50 of 8 nM.
PD158780 inhibits EGFR autophosphorylation in A431 human epidermoid carcinoma cells (IC50=15 nM).
PD158780 potently inhibits the LPA-stimulated MKK1/2 activation and EGFR phosphorylation in HeLa cells.
PD158780 also inhibits the kinase activity of ACK-1 in vitro (IC50=200 nM), inhibits the growth of v-Ha-Ras-transformed NIH 3T3 cells.
