The incidence and mortality of various tumors have been increasing, and the search for novel anti-tumor targets is one of the major research directions for anti-tumor drug development. Transient receptor potential canonical (TRPC) channels are a class of critical non-selective cation channels permeable to sodium (Na+ ), calcium (Ca2+ ), and other cations located on the cell membrane, which are widely distributed in vivo and participate in a variety of physiological and pathological processes. Studies have shown that the protein and mRNA levels of TRPCs are abnormally overexpressed in various tumor cells, which can promote tumor proliferation by increasing the intracellular Ca2+ concentration of tumor cells. Since TRPC receptors are located on the cell surface, ion channel-targeted drugs do not need to enter the cell, making them ideal therapeutic targets. Ca2+ , as one of the most essential intracellular messengers, plays a critical role in regulating cell growth and death, as well as tumor cell proliferation and apoptosis. Ca2+-permeable TRPC channels play a crucial role in tumor development, making them prognostic markers and potential therapeutic targets for malignant tumors. Targeting TRPC channels to regulate intracellular Ca2+ concentration and, in turn, modulate downstream signaling pathways is a novel approach to inhibiting tumor cell proliferation. This review summarizes the effects and mechanisms of TRPCs on tumorigenesis and development, and focuses on the potential of the extracellular small molecule binding pockets of the TRPC family as targets for anti-tumor small molecule compounds.