Pterostilbene, a natural dimethylated analog of resveratrol, exerts pleiotropic anticancer effects against a variety of cancer types. Due to the better lipophilic and oral absorption, higher cellular uptake and a longer half-life than resveratrol, pterostilbene may have a good prospect in the future clinic application. In this review, we summarize the previous in vitro and in vivo studies about the anticancer actions of pterostilbene on malignances, and we also evaluate the evidence related to the effects of pterostilbene on blocking normal cell carcinogenesis. Special focus is placed on the oncostatic effects of pterostilbene, including inhibition of tumor growth, metastasis, angiogenesis and cancer stem cells, activation of apoptosis, and enhancement of immunotherapy. We then clarify the emerging investigations about pterostilbene and chemotherapy and radiotherapy. Taken together, the information complied herein may serve as a comprehensive reference for the anticancer mechanisms of pterostilbene and may advance it as a future adjuvant therapeutic agent for cancer.