Table 2.

Reported potencies of dual PI3K/mTOR and pan-PI3K inhibitors against the 4 class I isoforms of PI3K

IC50 (nmol/L)
Inhibitor (ref.)PI3KαPI3KβPI3KγPI3KδmTOR
BEZ235 (78)4755721
GDC-0980 (4)52714717
GSK2126458 (79)0.0190.130.60.0024mTORC1: 0.18
mTORC2: 0.3
PF-05212384 (80)0.466 (81)81.6
SAR245409 (XL-765) (81)39113943mTORC1: 190
mTORC2: 908
Buparlisib (BKM120) (82)521662621164610
SAR245408 (XL-147) (83)393832336>15,000
Pictilisib (GDC-0941) (84)333753580
BAY80-6946 (85)0.53.76.40.7>1,000
PX-866 (86)3988183124>30,000

Abbreviations: IC50, half maximal inhibitory concentration; mTORC, mammalian target of rapamycin complex.