The fluorogenicity nature of HPPH enabled us to use the CPT‐TK‐HPPH/Pt NP as an outstanding probe to visualize cellular uptake in vitro, and tissue distribution in vivo via fluorescence imaging and photoacoustic imaging, which demonstrated the promoting accumulation of CPT‐TK‐HPPH/Pt NP in tumor sites. Here, TKT is linked to neoplasm.