This system has also been equipped with an aggregation-induced emission (AIE) behavior and a two-photon capability, enabling potential use for two-photon cell imaging and deep tissue imaging. Considerable cytotoxicity was shown on 4T1 cells and in vivo antitumor efficacy also assessed a higher tumor inhibition and less focal necrosis, liver and spleen inflammation compared to the use of free Gem, making this system promising for both cancer treatment and diagnosis.