Alpelisib (BYL719) is a potent inhibitor of PIK3CA (~5 nM), PIK3CG (~250 nM), PIK3CD (~290 nM), PIK3CB (~1200 nM), mTOR (>10 μM), and PI 4-kinase b (0.5 mM). Alpelisib (BYL719) exhibits the greatest inhibitory potency toward PIK3CA (IC50 = ~5 nM).
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