Tumor cell metabolism is characterized by abundant glucose consumption and aerobic glycolysis. And pyruvate kinase M2 (PKM2) plays a decisive role in glycolysis, significantly contributing to the Warburg effect, tumor growth, angiogenesis, cell division, metastasis and apoptosis. To date, researchers have unraveled the potential of pyruvate kinase M2 as an antitumor target, which suggests a new orientation for oncotherapy. Herein, we focus on the role of pyruvate kinase M2 in tumor cell development and its function as a potential new therapeutic target for tumor treatment. Besides, research actuality on pyruvate kinase M2-dependent glycometabolism and signaling pathway in tumors is also summarized, providing valuable suggestions for further study in this field.