© 2020, King Abdulaziz City for Science and Technology. Myricetin, one of the most extensively studied polyphenols, is present abundantly in various fruits and vegetables and exhibits diverse pharmacological properties. The multifaceted biological action of myricetin against tumor heterogeneity makes it an impressive anticancer agent whose efficacy has been confirmed by an overwhelming number of studies. Myricetin shows its therapeutic potential by targeting and modulating the expression of various molecular target which are involved in inflammation, cell proliferation, apoptosis, angiogenesis, invasion, and metastasis. Myricetin deters tumor progression by inducing apoptosis via both intrinsic and extrinsic pathway, activating/inactivating several signaling pathways, and reactivating various tumor suppressor genes. This comprehensive review represents the effect of myricetin on various hallmarks of cancer with insight into the molecular mechanism employed by myricetin to mitigate cell proliferation, angiogenesis, metastasis, and induce apoptosis. In addition, enhanced bioavailability of myricetin through conjugation and its increased efficacy as an anticancer agent when used in combination are also highlighted.