EGFR-IN-57 (Compound 25a) is a potent, orally active EGFR-TK inhibitor with an IC 50 of 0.054 µM. EGFR-IN-57 also inhibits VEGFR-2 , CK2α , topoisomerase IIβ and tubulin polymerization with IC 50 values of 0.087, 0.171, 0.13 and 3.61 µM, respectively. EGFR-IN-57 induces cell cycle arrest at G2/M and pre-G1 phases. EGFR-IN-57 induces cancer cell apoptosis.