Figure 1WZ4002, WZ3146 and WZ8040 are novel EGFR inhibitors, suppress the growth of EGFR T790M containing cell lines and inhibit EGFR phosphorylation
A. Chemical structures of the WZ compounds. B. IC50 values (nM) for NSCLC cell lines (top) and Ba/F3 (bottom) cells, with genotypes corresponding to the NSCLC cell lines, treated with indicated drugs. Growth was assessed using the MTS survival assay. C. Comparison of WZ3146, WZ4002 and CL-387,785 on EGFR signaling in PC9 GR cells. The cells were treated with the indicated concentrations of each drug for 16 hours. Cell extracts were immunoblotted to detect the indicated proteins. D. Comparison of EGFR inhibitors on EGFR phosphorylation in 3T3 cells expressing del E746_A750/T90M. The cells were treated with indicated concentrations of each drug for 16 hours and stimulated with EGF (10 ng/ml) 15 minutes prior to lysis. Cell extracts were immunoblotted to detect the indicated proteins.