PD 158780 is a potent tyrosine kinase inhibitor that can permeate cells and shows no inhibition against FGF or PDGF-mediated tyrosine phosphorylation. PD 158780 shows high specificity for inhibiting EGF-dependent autophosphorylation and can inhibit other members of the EGF-receptor family, such as Neuregulin-1 (heregulin)-stimulated phosphorylation. Research shows that PD 158780 can cause G1 cell cycle arrest through the inhibition of erbB family (EGFR, Neu, ErbB-3, and ErbB-4) receptor tyrosine kinase activity in the breast epithelial cell line MCF10A. Studies show that LPA-stimulated MAPK kinase activation and EGFR tyrosine phosphorylation in HeLa and NIH 3T3 cells can be inhibited by PD 158780. It has been observed that PD 158780 has anti-proliferative activity in A431 human epidermal carcinoma cells.
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