EGFR-IN-144 (Compound 4B) exhibits inhibitory activities against EGFR ( IC 50 =0.639 µg/mL) and tubulin polymerization ( IC 50 =7.339 µg/mL). EGFR-IN-144 exhibits cytotoxicity in multiple cancer cell with GI 50 of nanomolare levels. EGFR-IN-144 downregulates the expressions of mTOR , TNF-α, and IL-6 , arrests the cell cycle at G1/S phase, and induces apoptosis.