Table 1.
Summary of phosphoinositide-3 kinase inhibitors
| Study | Drug |
IC50 (nM)
|
|||||
|---|---|---|---|---|---|---|---|
| p110α | p110β | p110γ | P110δ | mTOR | Phase 1 trials | ||
| Ihle et al. [26]; Toral-Barza et al. [54] | Wortmannin | 2 | 0.6 | 10 | 3.9 | 200 | No |
| Garlich et al. [25], Toral-Barza et al. [54] | LY294002 | 720 | 306 | 1,600 | 1,330 | 1,500 | No |
| Ihle et al. [26] | PX-866 | 0.1 | > 300 | 1.0 | 2.9 | NA | Yes |
| Chiorean et al. [28] | PWT-458 | NAa | NAa | NAa | NAa | NAa | No |
| Garlich et al. [25]; Chiorean et al. [29] | SF1126 | NAb | NAb | NAb | NAb | NAb | Yes |
| Folkes et al. [30];Wagner et al. [31]; Sarker et al. [32] | GDC-0941 | 3 | 33 | 75 | 3 | 580 | Yes |
| Foster et al. [33]; Shapiro et al. [34]; Faulkner et al. [35]; Wheler et al. [36] | XL147 | 39 | 383 | 23 | 36 | 15,000 | Yes |
| Maira et al. [38] | NVP-BEZ235 | 4 | 75 | 5 | 7 | 21 | Yes |
| GDC-0980 | NA | NA | NA | NA | NA | Yes | |
| LoRusso et al. [37] | XL765 | 39 | 113 | 9 | 43 | 157 | Yes |
| Flinn et al. [43••] | CAL-101 | NA | NA | NA | 2.5 | NA | Yes |
a
PWT-458 is a pegylated form of wortmannin
b
SF1126 is a close derivative of LY294002
mTOR mammalian target of rapamycin, NA not available