Table 1.
EC50 values generated for hits from primary screen
| Pathway | Target | Drug | EC50 72 h (nM) | |
|---|---|---|---|---|
| SKLMS1 | STS39 | |||
| PI3K/AKT/mTOR | PI3K | PIK-75 | 10.79 | 14.9 |
| PIK-90 | 1705.3 | 952.2 | ||
| BKM120 | 800.0 | 513.2 | ||
| ZSTK474 | 149.0 | 318.8 | ||
| PF-04691502* | 59.3 | 57.0 | ||
| BEZ235* | 62.8 | 73.5 | ||
| AKT | A-443654 | 313.8 | 430.1 | |
| GSK-690693 | – | – | ||
| MK-2206 | 933.5 | 486.9 | ||
| mTOR | AZD-8055 | 12.1 | 12.61 | |
| OSI-027 | – | – | ||
| Everolimus | - | – | ||
| KU0063794 | 434.3 | 240.1 | ||
| Rapamycin | – | – | ||
| Cell cycle regulators G2/M | Chk 1 and 2 | AZD-7762 | 139.9 | 1001.0 |
| PLK1 | BI-2536 | 1922.0 | – | |
| GSK-461364 | 6.7 | – | ||
| BI-6727 (volasertib) | – | – | ||
| Cell cycle regulators G1/S | Wee-1 | MK-1775 | 40.0 | – |
| Other RTK | LIMK | LIM2K | – | – |
EC50 values generated by the 20 hits found in the primary screen for both STS39 and SKLMS1. The 10-point dilution curve includes doses ranging from 0.25 to 5000 nM. Highlighted boxes are inhibitors used in further studies. Inhibitors with dash (–) indicate no EC50 value was generated, * indicates a dual inhibitor targeting both PI3K and mTOR