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Nanotechnology has been widely applied in tumor imaging, diagnostic and therapy. Beside the prefabricated nanomaterials, constructing nanostructures in living cells through self-assemble provides an alternative strategy to treat cancer. In vivo self-assembly renders the conversion of compatible small molecules into assembled nanostructures with toxicity, and is expected to outperform the prefabricated nanotechnologies as the small molecules diffuse faster than their assembly form. Attributed to the specific tumor environment such as low