Abstract: Copper is an essential trace element in the human body, which participates in numerous cellular mechanisms and signaling pathways, and various biological activities need to be coordinated through redox activity of copper. If the amount of copper in the cell exceeds the cell's own needs or is improperly distributed within the cell, the cellular toxicity will occur, and many cancers will be characterized by increasing of copper. Copper can participate in the development and spread of cancer by promoting cell proliferation, angiogenesis, and cell metastasis. Copper chelators and copper ion carriers are effective means of maintaining copper concentration at physiological levels. This paper reviewed the regulation of copper in cells and the role of copper and copper binding proteins in the occurrence and development of cancer, and discussed the therapeutic progress of using copper derivatives as anticancer agents.