Fluorescence microscopy has emerged as an attractive technique to probe the intracellular processing of Pt-based anticancer compounds. Herein, we reported the first through-bond energy transfer (TBET) fluorescent probe NPR1 designed for sensitive detection and quantitation of Pt complexes. The novel TBET probe was successfully applied for ratiometric fluorescence imaging of anticancer Pt complexes such as cisplatin and JM118 in cells. Capitalizing on the ability of the probe to discriminate between Pt complexes and their Pt derivatives, the probe was further applied to study the activation of Pt prodrug complexes that are known to release active Pt species after intracellular reduction.
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