Theranostic Potential of an NAD(P)H‐Activatable Fluorophore: Assessing Cancer Aggressiveness and Triggering Apoptosis

Molecular theranostics, integrating precise diagnosis with targeted therapy, represents a cornerstone of personalized medicine. As a pivotal metabolic cofactor, reduced nicotinamide adenine dinucleotide (phosphate) (NAD(P)H) is intrinsically linked to cancer progression and survival when dysregulated. In this study, we report DE-CQ, an NAD(P)H-activatable fluorophore that enables both cancer imaging and apoptosis. DE-CQ allows the real-time quantification and visualization of intracellular NAD(P)H, serving as a robust molecular indicator of cancer malignancy. Beyond its diagnostic utility, DE-CQ preferentially induces mitochondria- and ER stress-dependent, caspase-mediated apoptosis in aggressive MDA-MB-231 cancer cells while maintaining minimal toxicity toward normal cells. Our findings demonstrate that DE-CQ functions as a potent theranostic agent, simultaneously providing diagnostic insights into cancer aggressiveness and triggering cell death. Given its dual functionality and high selectivity, DE-CQ holds significant potential as a next-generation platform for advanced, personalized cancer treatment.