Organotin (IV)-tetraphenylethylene (TPE) acylhydrazone compounds with aggregation-induced emission (AIE) property were prepared and characterized. The organotin (IV) compounds showed a conspicuous fluorescence improvement with a high absolute fluorescence quantum yield of 25.2 % (ClSnTPE) in the aggregation state, and restriction of intramolecular rotation (RIR) contributed to this AIE property. Using suitable fluorescence, confocal tests verified that these compounds could accumulate in the mitochondria of A549 cancer cells and decrease the mitochondrial membrane potential. Meanwhile, compounds could improve the intracellular reactive oxygen species (ROS) levels and inhibit the cell cycle (G1/G0 phase), then contributing to apoptosis. In addition to favorable in-vitro anti-proliferative activity (the similar to cisplatin), these compounds could also suppress A549 cancer cell migration. Above all, organotin (IV)-TPE acylhydrazone compounds show the promise as the mitochondrial targeting anticancer drugs for further study.