Cancer, a group of various diseases involving unregulated cell growth, it is a lifethreatening disease with an alarmingly increased annual mortality rate globally. Although various therapies are used for cancer treatment, the effect is not satisfactory. Chemotherapy is one of the most commonly used mothods of treatment. However, severe adverse reactions and drug resistance always influence the chemotherapy effect. Ginseng is traditional Chinese medicine, ginsenoside Rg3 is the main pharmacologically active component in ginseng and has been reported to have an antitumor effect, which was originally used in ancient times for the treatment of diseases. This review sheds light on the molecular mechanisms underlying the cancer chemotherapeutic activity of ginsenoside Rg3 with particular focus on the mechanism associated with cell proliferation, apoptosis, angiogenesis, inflammation and the metastasis of cancer cells. The review can enhance the understanding of the anticancer mechanisms of ginsenoside Rg3, provide directions for clinical practice and give more information for developing novel anticancer agents with high efficiency, low toxicity and weak resistance.