Potent steroid receptor coactivator 3 (SRC-3) inhibitor. Reduces SRC1, SRC2 and SRC3 levels in breast cancer cell lines. Inhibits cell growth (IC50 = 3.4 nM), induces apoptosis and attenuates migration of MDA-MB48 breast cancer cells in vitro. Inhibits tumor growth in a MDA-MB48 cell breast cancer mouse model. Orally available.
Song et al (2016) Development of potent small-molecule inhibitors to drug the undruggable steroid receptor coactivator-3. Proc.Natl.Acad.Sci.U.S.A. 113 4970 PMID:27084884