Table 2. Main PI3K inhibitors in clinical trials and their kinase inhibition profiles.
| Inhibitor | Structure | IC50 (μmol/L) p110α, p110β p110δ, p110γ | Isoform specificity | Selectivity over mTOR | Organization |
|---|---|---|---|---|---|
| CAL-101 |  |
>100 75 0.5 29 | PI3Kδ specific | Unknown | Calistoga |
| NVP-BEZ235 |  |
0.004 0.076 0.005 0.007 | Pan | No | Novartis |
| XL-765 | NA | 0.039 0.113 0.043 0.009 | Pan | No | Exelixis |
| GDC-0980 | NA | 0.005 0.027 0.007 0.014 | Pan | No | Genentech |
| SF1126 |  |
NA NA NA NA | Pan | No | Semafore |
| GSK-2126458 |  |
0.000019 0.00013 0.000032 0.000054 | Pan | No | GlaxoSmithKline |
| PX-866 |  |
0.006 >0.3 0.003 0.009 | Pan | Unknown | ProlX |
| BKM-120 |  |
0.052 0.166 0.116 0.262 | Pan | Yes | Novartis |
| XL-147 | NA | 0.039 0.383 0.036 0.023 | Pan | Yes | Exelixis |
| GDC-0941 |  |
0.003 0.033 0.003 0.075 | Pan | Yes | Genentech |
| ZSTK474 |  |
0.016 0.044 0.005 0.049 | Pan | Yes | Zenyaku |