CQ-Mito is a Coumarin-Quinazolinone (CQ)-based derivative that targets mitochondria and exhibits profound phototherapeutic performances with an Phototoxic Index ( PI ) value of 167. CQ-Mito causes cell death by both apoptosis and ferroptosis. CQ-Mito mediates mitochondrial dysfunction, including mitochondrial morphology changed and the loss of MMP. CQ-Mito can efficiently inhibit the tumor growth in organoid tumor models.