Abstract Self‐assembled functional supramolecular metallopolymers have demonstrated application potential in cancer therapy. Herein, a copper polypyridyl complex was found able to self‐assemble into a supramolecular metallopolymer driven by the intermolecular interactions, which could enhance the uptake in cancer cells through endocytosis, and thus effectively inhibiting tumor growth in vivo without damaging to the major organs. This study provides a facile way to achieve enhanced anticancer efficacy by using self‐assembled metallopolymers.
