Alpelisib is a potent and selective (IC50s = 7.4 nM PI3Kalpha, 2.2 µM PI3Kß, 1.2 µM PI3KIdelta, 50-fold selectivity against 442 tested kinases) PI3Kalpha inhibitor.1 Approved for use in the treatment of HR(+), HER2(-), PIK3CA-mutated breast cancer. Alpelisib has been used in combination with various chemotherapeutics to treat ovarian2, colorectal3, kidney4, bladder5, and head and neck6 cancers.
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