Ginseng has been used as a well-known traditional Chinese medicine since ancient times. Ginsenosides as its main active constituents possess a broad scope of pharmacological properties including stimulating immune function, enhancing cardiovascular health, increasing resistance to stress, improving memory and learning, developing social functioning and mental health in normal persons, and chemotherapy. Ginsenoside Rh2 (Rh2) is one of the major bioactive ginsenosides from Panax ginseng. When applied to cancer treatment, Rh2 not only exhibits the anti-proliferation, anti-invasion, anti-metastasis, induction of cell cycle arrest, promotion of differentiation, and reversal of multi-drug resistance activities against multiple tumor cells, but also alleviates the side effects after chemotherapy or radiotherapy. In the past decades, nearly 200 studies on Rh2 in the treatment of cancer have been published, however no specific reviews have been conducted by now. So the purpose of this review is to provide a systematic summary and analysis of the anticancer effects and the potential mechanisms of Rh2 extracted from Ginseng then give a future prospects about it. In the end of this paper the metabolism and derivatives of Rh2 also have been documented.Copyright © 2020 Elsevier Masson SAS. All rights reserved.