A panel of 12 EGFR inhibitors were screened for inhibition of EGFR phosphorylation in U87MG tumor cells engineered to express EGFR-viii. Compounds elicited a range of activity against phosphoY1173-EGFR. While one group of inhibitors had relatively weak activity against EGFR-viii (WZ4002, WZ8040, WZ3146, CO-1686, and AZD9291) another group had relatively potent activity against EGFR-viii (pelitinib, canertinib, PD168393, neratinib, AST-1306, and dacomitininb). The data described herein provide new methods of use for pelitinib, canertinib, AST-1306, and PD168393 against cancer, such as GBM, that express EGFR-viii. Furthermore, neratinib also exhibited selectivity towards splice variants EGFR-vii and EGFR-vvi compared to wild-type EGFR.
