Malignant tumors pose a serious threat to human life. Dual-functional agents with near-infrared fluorescence imaging and photodynamic therapy (PDT) activities have significant potential for synchronous cancer diagnosis and treatment due to their high sensitivity and noninvasiveness. In this study, based on the "organelle-targeted PDT" strategy, we developed a mitochondria-targeted and endoplasmic reticulum (ER)-located fluorescent probe,