GW2974

GW2974 is a dual selective inhibitor of EGFR and Neu (ErbB-2) receptor tyrosine kinases. It is known that tyrosine kinases are transmembrane proteins, which are essential in cell growth and survival. Studies indicate that GW2974 inhibits cancer line PC-3 growth, via its ability to inhibit tyrosine kinases. In addition, GW2974 stimulates the amount of NSE and Chr-A (chromogranin A) in cells. Studies involving BK5.erbB2 mice show that GW2974 inhibits 12-O-tetradecanoylphorbol-13-acetate-induced epidermal hyperproliferation, which resulted in a lower expression of EGFR and Neu. Furthermore, these studies suggest that the inhibitory effects on cell growth of GW2974 is more potent during tumor promotion and when Neu is overexpressed.