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Theranostics is an emerging technique for cancer treatments due to its safety and high efficiency. However, the stability, efficiency, and convenience of preparation are the main challenges for developing theranostics. Here we describe a one-pot process for biocompatible metal–organic framework (MOF)-based theranostics. The ligand H2L designed for the MOF enables both red fluorescence emission and photodynamic therapy (PDT). The frame and regular channel structure of H2L-MOF empower the theranostics with good drug delivery performance, and the uniform and nano-sized particles facilitate the in vivo imaging/therapy applications. In vivo fluorescence imaging and in vitro chemo-photodynamic therapy were achieved with the MOF without any further modification. Our results reveal an effective strategy to achieve multifunctional theranostics by the synergistic action of the organic ligand, metal node, and channel structure of MOF nanoparticles.

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