Table 2.
IC50 values for inhibition of ALK Y1604 phosphorylation in the context of full‐length ALK expressed in PC12 cells by either brigatinib, lorlatinib, ceritinib or crizotinib
| ALK mutation | ALK TKI IC50s | ||||
|---|---|---|---|---|---|
| Brigatinib | Lorlatinib | Ceritinib | Crizotinib* | Crizo SD* | |
| Wildtype | 2.60 | 0.80 | 5.30 | 16.40 | 4.17 |
| G1128A | 2.00 | 1.20 | 19.80 | 33.53 | 10.15 |
| I1171N | 10.30 | 3.20 | 46.60 | 97.53 | 50.00 |
| I1171T | 7.50 | 6.80 | 17.40 | 193.00 | |
| F1174L | 1.50 | 0.70 | 17.00 | 23.16 | 5.8 |
| R1192P | 2.50 | 0.90 | 26.10 | 42.50 | 19.95 |
| F1245V | 6.60 | 0.90 | 24.70 | 32.02 | 6.78 |
| G1269A | 3.40 | 6.40 | 29.80 | 130.13 | 24.11 |
| R1275Q | 4.20 | 0.80 | 10.80 | 30.63 | 1.72 |
| Y1278S | 4.60 | 2.30 | 20.50 | 53.7 | 29.91 |
ALK, anaplastic lymphoma kinase; TKI, tyrosine kinase inhibitor.
The table is compiled from three independent articles, all of which have employed investigated crizotinib for comparison with other ALK TKIs 120, 132, 140. Crizotinib* indicates average of crizotinib treatment based on these studies and crizo* SD indicates standard deviation of these values. Results for ALK‐I1171T are taken from 120.