Cellular IC90 values of Bcr-Abl resistance mutations identified in the nilotinib screen
Mutation . | Nilotinib, nM . | Fold, IC90 wt . |
|---|---|---|
| Wild-type p185 | 87 | NA |
| Q252H | 383 | 4.4 |
| Y253H | 2640 | 30.2 |
| E255K | 644 | 7.4 |
| E255V | 1928 | 22.1 |
| F311I | 467 | 5.4 |
| T315I | > 4000 | > 45 |
| S349L | 119 | 1.4 |
| S349L + Q252H | 887 | 10.2 |
| F359I | 433 | 5 |
| F359V | 682 | 7.8 |
Mutation . | Nilotinib, nM . | Fold, IC90 wt . |
|---|---|---|
| Wild-type p185 | 87 | NA |
| Q252H | 383 | 4.4 |
| Y253H | 2640 | 30.2 |
| E255K | 644 | 7.4 |
| E255V | 1928 | 22.1 |
| F311I | 467 | 5.4 |
| T315I | > 4000 | > 45 |
| S349L | 119 | 1.4 |
| S349L + Q252H | 887 | 10.2 |
| F359I | 433 | 5 |
| F359V | 682 | 7.8 |
Ba/F3 cells were transfected with engineered mutant forms of Bcr-Abl and treated as stated in Figure 4. IC90 values and fold increase in comparison to Bcr-Abl wild type-expressing Ba/F3 cells were calculated using the resulting growth curves.
NA indicates not applicable.