Table 3.
mTORC1/mTORC2 dual inhibitors in vitro kinase IC50 (nM)
| PP242 [31] | PP30 [31] | WAY600 [34] | WYE687 [34] | WYE354 [34] | WYE132 [35] | AZD8055 [37] | Ku0063794 [42] | |
|---|---|---|---|---|---|---|---|---|
| mTOR | 8 | 80 | 9 | 7 | 5 | 0.19 ± 0.07 | 0.8/0.13 | 3/16 |
| PI3Kα | 1960 | 3000 | 1960 | 810 | 1890 | 1179 | 3590 | 8900 |
| PI3Kβ | 2200 | 5800 | n.d. | n.d. | n.d. | >10000 | 18900 | >30000 |
| PI3Kγ | 1270 | 990 | 8450 | 3110 | 7370 | >10000 | >14790 | >30000 |
| PI3Kδ | 102 | 680 | n.d. | n.d. | n.d. | 2380 | 3200 | >5300 |
| DNA-PK | 408 | 339 | n.d. | n.d. | n.d. | n.d. | 1370 | >10000 |
| Chemical structure | ![]() |
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| Inventor | Intellikine | Intellikine | Wyeth | Wyeth | Wyeth | Wyeth | AstraZeneca | AstraZeneca |
n.d., not determined.







