In this study, it is found that by optimizing the experimental conditions, EphA2-localized TPE-Py-FFGYSA can provide an intracellular oxidative environment through the light controlled generation of ROS without killing the cancer cells, which dramatically enhances the cytotoxicity of Ptx against PC-3 cancer cells, achieving the synergistic effect of “0 + 1 > 1”. This evidence concerns the gene EPHA2 and cancer.