Table 1.
Inhibitor | Structure | IC50 (nmol/L) |
Isoform specificity | Selectivity over mTOR | Organization (development status) | |||
---|---|---|---|---|---|---|---|---|
p110α | p110β | p110δ | p110γ | |||||
Idelalisib | 820 | 565 | 2.5 | 89 | p110δ specific | unknown | Gilead (launched) | |
IPI-145 | 1602 | 85 | 3 | 27 | PI3Kδ, γ specific | unknown | Infinity Pharmaceuticals (phase III) | |
NVP-BEZ235 | 4 | 76 | 5 | 7 | pan | No | Novartis (phase I) | |
BKM-120 | 52 | 166 | 116 | 262 | pan | Yes | Novartis (phase III) | |
BYL-719 | 5 | 1200 | 290 | 250 | PI3Kα specific | Yes | Novartis (phase III) | |
GDC-0941 | 3 | 33 | 3 | 75 | pan | Yes | Genentech (phase I) | |
GDC-0980 | 5 | 27 | 7 | 14 | pan | No | Genentech (phase II) | |
SF1126 | NA | NA | NA | NA | pan | No | SignalRx (phase I) | |
PX-866 | 6 | >300 | 3 | 9 | pan | unknown | Oncothyreon (phase II) | |
PF-04691502 | 1.8a | 2.1a | 1.6a | 1.9a | pan | No | Pfizer (phase I) | |
BAY-80-6946 | 0.5 | 3.7 | 6.4 | 0.7 | pan | Yes | Bayer (phase III) | |
XL-765 | 39 | 113 | 43 | 9 | pan | No | Sanofi (phase I/II) | |
XL-147 | 39 | 383 | 36 | 23 | pan | Yes | Sanofi (phase I) | |
GSK2126458 | 0.019 | 0.13 | 0.024 | 0.06 | pan | No | GlaxoSmithKline (phase I) | |
ZSTK474 | 16 | 44 | 5 | 49 | pan | Yes | Zenyaku (phase I/II) |
NA, not available.
Ki.