Abstract: Casticin is a flavonoid that is derived from the Vitex species. Multiple studies have investigated the anticancer properties of casticin against many types of cancer, such as bladder cancer, breast cancer, oral cancer, lung cancer, and leukemia. Research has shown the ability of casticin to inhibit cell growth and induce programmed cell death. The chemical exhibits efficacy against numerous cancer cell lines through various molecular mechanisms. The substance hinders the processes of invasion, migration, and proliferation and triggers programmed cell death by multiple mechanisms, including the generation of reactive oxygen species and the dependence on mitochondria. Additionally, it inhibits the cell cycle at different stages. These effects are achieved by modulating several signaling cascades, specifically NF-κB, PI3K/Akt, FOXO3a/FoxM1, and STAT3. This review provides a concise overview of the chemotherapeutic efficacy of casticin as an anticancer drug.