The invention relates to a chlorin and artesunate compound with photosensitive and sound-sensitive activity as well as a preparation method and an application of the compound and belongs to the technical field of chemical medicines. The chlorin and artesunate compound with photosensitive and sound-sensitive activity has different degrees of inhibition effects on human hepatoma cells Hep G2 in in-vitro anti-tumor activity evaluation. The photoactivity and ultrasonic activity are both higher than that of chlorin e6 and artesunate which are used as positive controls. The compound can be used for preparing a photosensitizer and a sound-sensitive agent in photodynamic therapy and sonodynamic therapy methods for tumor therapy.