Cancer is a life-threatening disease with an alarmingly increased annual mortality rate globally. Although various therapies are employed for cancer, the final effect is not satisfactory. Chemotherapy is currently the most commonly used treatment option. However, the unsatisfactory efficacy, severe side-effects and drug resistance hinder the therapeutic efficacy of chemotherapeutic drugs. There is increasing evidence indicating that ginsenoside Rg3, a naturally occurring phytochemical, plays an important role in the prevention and treatment of cancer. The suggested mechanisms mainly include the induction of apoptosis, and the inhibition of proliferation, metastasis and angiogenesis, as well as the promotion of immunity. In addition, ginsenoside Rg3 can be used as an adjuvant to conventional cancer therapies, improving the efficacy and/or reducing adverse effects via synergistic activities. Ginsenoside Rg3 may be a widely applied natural medicine against cancer. To date however, there is no systematic summary available of the anticancer effects of ginsenoside Rg3. Therefore, in this review, all available literature over the past 10 years was reviewed and discussed in order to facilitate further research of ginsenoside Rg3.