Photo-physical characteristics of fluorophore dyes such as Bodipy are regulated through some strategies such as π structure and noble metal coordination, and then these dyes are further assembled into mono-dispersive cancer-targeted nanoparticles such as micelles for causing ultralow radiative transition, accompanying with enhanced singlet oxygen quantum yield and higher photothermal conversion efficiency. Thus, the nanoparticles are able to generate synergistic photodynamic and photothermal therapy for tumor ablation without any regrowth.