EGFR/COX-2-IN-3 is a selective EGFR / COX-2 dual inhibitor with IC50 values of 0.098 μM and 0.05 μM, respectively. EGFR/COX-2-IN-3 is predicted to have oral activity and blood-brain barrier permeability. EGFR/COX-2-IN-3 exhibits both potent analgesic activity and anti-glioblastoma effects. EGFR/COX-2-IN-3 can be used in the research of tumors such as glioblastoma [1].
In Vivo, EGFR/COX-2-IN-3 exhibits analgesic activity in the mouse hot-plate test, with an AUC of 37.83, which is superior to that of Celecoxib [1].
In Vitro, EGFR/COX-2-IN-3 (Compound 10a) exhibits potent cytotoxicity against U-251 and SNB-75, with IC50 values of 8.8 μM and 2.6 μM, respectively[1].
References:
[1]. Farag KO, et al. Pyrazole derivatives as dual COX-2/EGFR inhibitors with anticancer potential: Optimization of difenamizole Analogs. Bioorg Chem. 2026;170:109444.
In Vivo, EGFR/COX-2-IN-3 exhibits analgesic activity in the mouse hot-plate test, with an AUC of 37.83, which is superior to that of Celecoxib [1].
In Vitro, EGFR/COX-2-IN-3 (Compound 10a) exhibits potent cytotoxicity against U-251 and SNB-75, with IC50 values of 8.8 μM and 2.6 μM, respectively[1].
References:
[1]. Farag KO, et al. Pyrazole derivatives as dual COX-2/EGFR inhibitors with anticancer potential: Optimization of difenamizole Analogs. Bioorg Chem. 2026;170:109444.