Cancer is an unexpected consequence of uncontrolled cell proliferation that is related to cell cycle disorganization, and a multifactor-caused disease that needs the modulation of numerous oncogenic signaling pathways and targets. The battle with this malignance has been waged for centuries whereas this dreadful disease is still an important cause of death all over the world. Due to the development of resistance to current anticancer drugs, lots of efforts are made to discover more effective agents for tumor therapy. Meanwhile, natural products possess a powerful prospect for anticancer drugs discoveries. Brusatol, a component isolated from natural plant Brucea javanica, was able to efficiently combat with wide variety of tumors. Extensive researches had shown that Brusatol exhibited its anticancer capability by arresting cell cycle, promoting apoptosis, inducing autophagy, attenuating epithelial-mesenchymal transition, inhibiting migration, invasion and angiogenesis as well as raising chemosensitivity and radiosensitivity. In addition, these involved various oncogenic signaling pathways, including MAPK, NF-κB, PI3K/AKT/mTOR, JAK/STAT and Keap1/Nrf2/ARE signaling pathway. The current review describes in detail and discusses the various reports supporting the possibility of Brusatol to be a hopeful drug candidate for cancer therapeutics.