Decrease in sensitivity of mutants to imatinib, relative to wild type, compiled from this and other studies*
Mutation . | Biochemical sensitivity (fold decrease over wild type) . | Cellular sensitivity (fold decrease over wild type) . |
|---|---|---|
| Wild type | 1.0 | 1.0 |
| M244V* | 1.0 | 3.2 |
| G250E | 9 to >17 | |
| Q252H | 5.2 to 9.3 | |
| Y253F | 72 | 10 to 15 |
| Y253H | 150 | >33 |
| E255K | >200 | 15 to 33 |
| E255V | >200 | >33 |
| F311L† | 1.0 | 1.4 |
| T315I | >200 | >33 |
| F317L | 8.3 | 2.6 to 13 |
| M351T | 3.1 to 7.3 | |
| E355G | 0.8 | 4.0 |
| F359V† | 1.8 | 2.8 |
| V379I† | 1.1 | 2.0 |
| L387M† | 2.1 | 2.2 |
| H396P | 11 | 8.6 to 10 |
| H396R | 7.3 | 11 |
Mutation . | Biochemical sensitivity (fold decrease over wild type) . | Cellular sensitivity (fold decrease over wild type) . |
|---|---|---|
| Wild type | 1.0 | 1.0 |
| M244V* | 1.0 | 3.2 |
| G250E | 9 to >17 | |
| Q252H | 5.2 to 9.3 | |
| Y253F | 72 | 10 to 15 |
| Y253H | 150 | >33 |
| E255K | >200 | 15 to 33 |
| E255V | >200 | >33 |
| F311L† | 1.0 | 1.4 |
| T315I | >200 | >33 |
| F317L | 8.3 | 2.6 to 13 |
| M351T | 3.1 to 7.3 | |
| E355G | 0.8 | 4.0 |
| F359V† | 1.8 | 2.8 |
| V379I† | 1.1 | 2.0 |
| L387M† | 2.1 | 2.2 |
| H396P | 11 | 8.6 to 10 |
| H396R | 7.3 | 11 |
Where different studies report different values, a range is given. For space considerations, single-letter amino acid codes are used here in place of 3-letter codes.
Hochhaus et al,8 Corbin et al,10 Shah et al,16 and von Bubnoff et al.17
Mutants whose cellular IC50 values are near or below reported trough levels of imatinib (1.46 μM) in patients treated with 400 mg4 .