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For the first time, an AIEgen-conjugated monoclonal antibody is designed for “turn-on” and “wash-free” imaging of EGFR-overexpressed cancer cells., An antibody–AIEgen conjugate is designed and developed as a “turn-on” fluorescent probe for wash-free specific cancer cell imaging. The cetuximab-conjugated AIEgen shows red fluorescence only when it is internalized and accumulated in cancer cells with overexpressed epidermal growth factor receptor through endocytosis. The probe first lights up the lysosomes. After hydrolysis, its residue is accumulated in mitochondria, making them highly emissive with a long cell retention time. Compared with conventional “always-on” fluorescent probes, the antibody–AIEgen conjugate exhibits a very good image contrast during wash-free cancer cell imaging and less interference from normal cells. To the best of our knowledge, this is the first time “turn-on” antibody–AIEgen conjugates have been reported. This new strategy can be further extended to many proteins and water-soluble AIEgens, and many of their potential applications such as real-time tracking of cell dynamics and cancer theranostics will be explored. The present work is expected to inspire more marvellous research in the fields of AIE and cancer imaging.

Two azide-functionalized tetraphenylethene derivatives with AIE features are synthesized and used as fluorescent agents for detecting S-phase DNA synthesis and cell proliferation based on EdU assay. Compared to the Alexa-azide dye, a commercial DNA bioprobe, the AIE fluorogens show better photostability and sensitivity, making them promising alternatives.