Targeted copper supplementation oriented theranostic for fluorescence and ¹⁹F NMR detection of tumors

Alteration of the levels of copper is a promising approach for cancer therapy. Herein, we develop a dual-mode copper vehicle, M985. The biotin-tailed M985 can exert tumor-directed copper supplementation and undergo self-immolative cleavage in living cancerous cells, resulting in the liberation of F542 along with the generation of excess reactive oxygen species. Thus, fluorescence and 19F NMR detection is realized to specifically discriminate cancer cells. F542 acts as a fluorescence reporter and a potent cytotoxic agent, facilitating the visualization of molecular release and distribution, as well as confirming the ER autophagy-induced apoptosis. Therefore, we present a promising dual-mode theranostic M985 for the efficient detection and therapy of cancer.