Summary of Ba/F3 cell proliferation experiments
. | Imatinib . | Nilotinib . | Dasatinib . | |||
---|---|---|---|---|---|---|
IC50, nM . | SEM . | IC50, nM . | SEM . | IC50, nM . | SEM . | |
Ba/F3 | > 2000 | NA | > 2000 | NA | > 100 | NA |
p210 | 406 | 51 | 34.3 | 2.8 | 2.53 | 0.49 |
Patient mutants | ||||||
N231D | 401 | 50 | 38.2 | 3.8 | 3.35 | 0.78 |
T212R | 957 | 96 | 84.4 | 5.6 | 3.75 | 0.36 |
A196V | 381 | 55 | 30.4 | 2.8 | 2.62 | 0.52 |
S154N | 256 | 69 | 28.3 | 6.9 | 2.61 | 0.64 |
K84N | 396 | 34 | 35.8 | 3.2 | 3.15 | 0.74 |
R47C | 392 | 46 | 33.2 | 3.1 | 2.71 | 0.56 |
E123Q | 510 | 33 | 35.7 | 3.6 | 1.98 | 0.18 |
N231I | 340 | 70 | 38.2 | 5.8 | 2.24 | 0.33 |
G144E | 373 | 44 | 39.1 | 3.7 | 2.89 | 0.39 |
Activating mutants | ||||||
Abl PP | 378 | 72 | 49.0 | 4.0 | 3.86 | 1.05 |
K51A | 433 | 68 | 38.0 | 5.5 | 4.00 | 1.21 |
W99A | 423 | 137 | 45.3 | 137.1 | 4.18 | 0.97 |
Y139D | 430 | 71 | 45.7 | 5.8 | 5.48 | 2.20 |
In vitro screen mutants | ||||||
T224A | 559 | 66 | 39.1 | 2.7 | 2.57 | 0.30 |
T212R double mutants | ||||||
E275K | 1343 | 134 | 116.5 | 16.4 | 3.19 | 0.36 |
T212R/E275K | ∼ 2000 | NA | 176.3 | 10.4 | 4.67 | 1.39 |
T212R/S154N | 403 | 73 | 36.6 | 1.8 | 1.79 | 0.19 |
. | Imatinib . | Nilotinib . | Dasatinib . | |||
---|---|---|---|---|---|---|
IC50, nM . | SEM . | IC50, nM . | SEM . | IC50, nM . | SEM . | |
Ba/F3 | > 2000 | NA | > 2000 | NA | > 100 | NA |
p210 | 406 | 51 | 34.3 | 2.8 | 2.53 | 0.49 |
Patient mutants | ||||||
N231D | 401 | 50 | 38.2 | 3.8 | 3.35 | 0.78 |
T212R | 957 | 96 | 84.4 | 5.6 | 3.75 | 0.36 |
A196V | 381 | 55 | 30.4 | 2.8 | 2.62 | 0.52 |
S154N | 256 | 69 | 28.3 | 6.9 | 2.61 | 0.64 |
K84N | 396 | 34 | 35.8 | 3.2 | 3.15 | 0.74 |
R47C | 392 | 46 | 33.2 | 3.1 | 2.71 | 0.56 |
E123Q | 510 | 33 | 35.7 | 3.6 | 1.98 | 0.18 |
N231I | 340 | 70 | 38.2 | 5.8 | 2.24 | 0.33 |
G144E | 373 | 44 | 39.1 | 3.7 | 2.89 | 0.39 |
Activating mutants | ||||||
Abl PP | 378 | 72 | 49.0 | 4.0 | 3.86 | 1.05 |
K51A | 433 | 68 | 38.0 | 5.5 | 4.00 | 1.21 |
W99A | 423 | 137 | 45.3 | 137.1 | 4.18 | 0.97 |
Y139D | 430 | 71 | 45.7 | 5.8 | 5.48 | 2.20 |
In vitro screen mutants | ||||||
T224A | 559 | 66 | 39.1 | 2.7 | 2.57 | 0.30 |
T212R double mutants | ||||||
E275K | 1343 | 134 | 116.5 | 16.4 | 3.19 | 0.36 |
T212R/E275K | ∼ 2000 | NA | 176.3 | 10.4 | 4.67 | 1.39 |
T212R/S154N | 403 | 73 | 36.6 | 1.8 | 1.79 | 0.19 |
NA indicates not applicable.