Table 3.
Characteristics (left) and sensitivity (right) to gefitinib and barasertib of the 11–18 derived cell lines used in the study
| Cell line | Doubling time (h) | EGFR L858R | EGFR T790M | EGFR overexpression | AXL overexpression | MET activation | FGFR1 overexpression | NRAS amplification (fold) | NRAS mutations Q61L/R/K | Gefitinib (EGFR) IC50 (µM) | Barasertib(AURKB) IC50 (µM) |
|---|---|---|---|---|---|---|---|---|---|---|---|
| 11–18 | 23 ± 4 | + | − | − | − | − | − | 4 | − | 0.2 | >50 |
| 11–18 GR1 | 27 ± 4 | + | − | + | − | − | − | 5 | 22% (Q61R) | 27.1 | 13 |
| 11–18 GR2 | 25 ± 2 | + | − | + | − | + | − | 4 | 9% (Q61L) | 8.0 | >50 |
| 11–18 GR3 | 24 ± 2 | + | − | + | − | − | − | 4 | − | 27.4 | 0.06 |
| 11–18 GR4 | 22 ± 1 | + | − | + | − | + | ++ | 5 | 4% (Q61L) | 20.6 | 14 |
| 11–18 GR5 | 27 ± 4 | + | − | + | − | − | − | 3 | − | 20.8 | 0.06 |
| 11–18 GR6 | 22 ± 1 | + | − | + | ++ | − | − | 4 | 9% (Q61K) | 8.1 | 18 |
The targets of the drugs are indicated between parentheses. Doubling times are expressed as means ± SD of at least three different determinations