Abstract: Small molecular inhibitors that selectively target cancer cells instead of normal cells are promising anti-cancer therapeutics. The mammalian target of rapamycin complex 2 ( mTORC2 ) is emerging as a potential target for inhibitors. Recent studies in oncobiology have indicated that the mTORC2 activity is essential for the transformation, as well as the vitality, of a number of cancer cell types, and that the mTORC2 inhibitor has a broad impact on cancer therapy. In the present study, new findings on the biology of mTORC2 signaling are summarized, and future prospects for mTOR-targeted therapy are highlighted.