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EGFR-IN-45 is a potent pan-inhibitor of the epidermal growth factor receptor (EGFR), acting on EGFR (IC50: 0.4 μM) and CDK2 (IC50: 1.6 μM). EGFR-IN-45 also inhibits the topoisomerases Topo I and Topo II. EGFR-IN-45 blocks the cell cycle of cancer cells in the pre-G1 phase and induces apoptosis.