Organelle-targeted two-photon near-infrared photosensitizers are highly desirable for photodynamic therapy (PDT) of cancer. Herein, in this contribution, we have developed a 2-dicyanomethylenethiazole-based D-π-A structured near-infrared photosensitizer (TTR). TTR exhibits near-infrared emission (704 nm), a large Stokes shift (200 nm), and smaller ΔE- (the energy gap between S and T) (0.717 eV). In vitro results show that TTR can specifically target lysosomes in living cells for near-infrared fluorescence imaging. With efficient ROS generation, excellent biocompatibility, two-photon imaging capability, and depth imaging (21 μm in vitro and 210 μm in vivo), TTR can effectively kill tumor cells and inhibit the growth of subcutaneous tumors. The hematoxylin-eosin (H&E) staining and blood biochemical parameter results further prove the biocompatibility of TTR. Hence, TTR can be a promising photosensitizer for PDT.
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