Table 2 Activity of ALK inhibitors (IC50, nM) on EML4::ALK-transfected Ba/F3 cells, wild-type (WT) or mutant.
IC50 [nM] | Crizotinib | Brigatinib | Ceritinib | Alectinib | Lorlatinib | Zotizalkib | Repotrectinib |
|---|---|---|---|---|---|---|---|
WT | 90 | 30 | 37 | 19 | 1.8 | 7.1 | 67 |
E1154K | 205 | 46 | 129 | 13 | 4.6 | 7.6 | 64 |
F1174L | 199 | 57 | 484 | 19 | 5.7 | 53 | 227 |
L1196P | 2140 | 3112 | 1798 | >3000 | 1854 | 338 | 1061 |
L1198R | 230 | 207 | 106 | 59 | 7.6 | 7.2 | 57 |
T1211I | 32 | 19 | 23 | 4.7 | 0.4 | 7.0 | 66 |
D1232N | 45 | 20 | 18 | 8 | 1.4 | 7.0 | 31 |
C1235R | 191 | 33 | 110 | 50 | 1.8 | 8.0 | 42 |
C1237Y | 1230 | 330 | >10,000 | >3000 | 1051 | 274 | 488 |
E1154K + F1174L | 159 | 59 | 324 | 40 | 5.8 | 31 | 100 |
L1196M + G1202Ra | 2401 | 1429 | 1826 | 2461 | 1964 | na | na |