Table 1. IC50 values for inhibition of ALK Y1604 phosphorylation by brigatinib or crizotinib in PC12 cells.
ALK mutations | IC50 (nM) | Fold difference | |
---|---|---|---|
brigatinib | crizotinib | ||
WT | 2.6± 0.2 | 19.68 ± 9 | 8 |
G1128A | 2.0 ± 0.6 | 41.82 ± 5 | 21 |
I1171N | 10.2 ± 5.7 | 110.90 ± 18 | 11 |
F1174L | 1.5 ± 0.4 | 25.35 ± 10 | 17 |
R1192P | 2.5 ± 0.4 | 64.0 ± 12 | 26 |
F1245C | 6.6 ± 0.3 | 34.07 ± 0 | 5 |
G1269A | 3.4 ± 2.0 | 118.9 ± 23 | 35 |
R1275Q | 4.2 ± 0.7 | 32.58 ± 0 | 8 |
Y1278S | 4.6 ± 0.2 | 72.44 ± 2 | 16 |
IC50 values were determined by quantification of Y1604 phosphorylation from the immunoblots in Figure 2A and 2B. Values represent mean ± SD from at least two independent experiments.