GDC-0980, a selective, potent, orally bioavailable inhibitor of Class I PI3 kinase and mTOR kinase (TORC1/2). It inhibits PI3Kα/β/δ/γ with IC₅₀ values of 5 nM/27 nM/7 nM/14 nM, respectively and mTOR with Ki of 17 nM. GDC-0980 is highly selective versus others PIKK family kinases. Displays anticancer activity.