IC50 values, expressed in μmol/L, obtained for each Ba/F3 cell line and relative therapeutic index (TI) calculated as IC50 parental line/IC50 mutant, are summarized
| CRIZOTINIB | AP26113 | NVP-TAE684 | |||||||
|---|---|---|---|---|---|---|---|---|---|
| IC50 | Norm | T.I. | IC50 | Norm | T.I. | IC50 | Norm | T.I. | |
| Ba/F3 | 1.261 | 36.090 | 1.000 | 0.820 | 78.021 | 1.000 | 0.760 | 127.389 | 1.000 |
| Ba/F3 NA WT | 0.035 | 1.000 | 36.090 | 0.011 | 1.000 | 78.021 | 0.006 | 1.000 | 127.389 |
| Ba/F3 L1196Q | 0.212 | 6.076 | 5.940 | 0.009 | 0.856 | 91.111 | 0.009 | 1.509 | 84.444 |
| Ba/F3 I1171N | 0.215 | 6.156 | 5.862 | 0.329 | 31.256 | 2.496 | 0.759 | 127.254 | 1.001 |
| Ba/F3 L1196M | 0.459 | 13.125 | 2.750 | 0.042 | 3.983 | 19.589 | 0.018 | 3.022 | 42.152 |
NOTE: IC50 values obtained derive from at least 2 independent experiments.