Here we have designed and synthesized a novel analogous cis-platinum complex (TDPt) with strong two-photon absorption properties and higher stability upon laser irradiation. Interestingly, a higher cytotoxicity against three types of cancer cells compared to that of commercial cis-platinum was observed. The initial confocal micrographs showed that lysosomes may be the biological targets of such TDPt, except the conventional presumed DNA. This hypothesis was further confirmed by the two-photon microscopy and transmission electron microscopy micrograph. These results form an important basis for future "on-site observation" of the anticancer mechanism of the Pt(II) complex.