Resveratrol (3, 5, 4'-trihydroxy-trans-stilbene, RVT), a stilbenoid, polyphenol phytochemical present in berries, grape, peanuts and wine. It has been suggested as a major contributor to "French Paradox" that reduces the mortality from coronary heart disease (CHD) by consuming RVT in red wine even in some of French population with a high-fat intake. With extensive research, it has been found that RVT is a versatile and pleiotropic agent, it not only possesses cardiovascular-protective benefits by its powerful antioxidant capacity, anti-inflammatory, regulating metabolism and anti-aging effects, but also has strong anti-tumor activities through inhibiting tumor cell proliferation, inducing cell apoptosis, promoting tumor cell differentiation, preventing tumor invasion and metastasis, and further moderating the host immune system to kill tumor cells. This review will focus on RVT's anti-tumor activity and tumor prevention potential including: the anti-tumor spectrum in vitro and in vivo; molecular targets and signal pathways involving RVT anti-tumor mechanisms; evidences from clinical trial for its bioavailability, dosage, toxicity and benefit in humans; and its prospective including its analog, deviations, and combinative chemotherapy.