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Herein, we report a mitochondria\u2010targeted prodrug system that integrates an AIE fluorophore with excited\u2010state intramolecular proton transfer (ESIPT) characteristics, covalently linked to the anticancer drug dasatinib. The amphiphilic prodrug self\u2010assembled into nanoparticles of around 210\u00a0nm with a spherical morphology. The probe is initially non\u2010fluorescent due to ESIPT inhibition. Following cellular internalization, intracellular esterases cleave the carbonate linker, initiating two simultaneous processes: (1) the cytosolic release of dasatinib to inhibit proliferation\u2010associated tyrosine kinases, and (2) the restoration of ESIPT and subsequent aggregation of the fluorophore, yielding a ratiometric fluorescence turn\u2010on signal for real\u2010time monitoring. The liberated probe, appended with a triphenylphosphine moiety, then selectively targets mitochondria, where it generates reactive oxygen species (ROS), inducing mitochondrial damage and promoting apoptosis. This combination of cytosolic kinase inhibition and mitochondria\u2010targeted ROS production creates a powerful synergistic anticancer effect, demonstrating significantly enhanced efficacy over dasatinib alone. This multifunctional design pioneers a theranostic approach that merges precise drug activation, dynamic imaging, and organelle\u2010specific therapy.<\/jats:p>","DOI":"10.1002\/asia.70885","type":"journal-article","created":{"date-parts":[[2026,8,16]],"date-time":"2026-08-16T05:56:33Z","timestamp":1786859793000},"update-policy":"https:\/\/doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":0,"title":["Mitochondria\u2010Targeted Cancer Therapy Using an Endogenous Stimuli\u2010Responsive Prodrug With Aggregation\u2010Induced\u2010Emission Features"],"prefix":"10.1002","volume":"21","author":[{"given":"Priyanka","family":"Patra","sequence":"first","affiliation":[{"name":"CSIR\u2010Central Salt and Marine Chemicals Research Institute Bhavnagar Gujarat India"},{"name":"Academy of Scientific and Innovative Research (AcSIR) Ghaziabad 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