FLT3 JM point mutants expressed in Ba/F3 cells are sensitive to the FLT3 PTK inhibitor PKC412
Mutation class . | IC50 PKC412, nM . |
|---|---|
| FLT3-ITD | |
| W51 | 5.0 |
| FLT3-TKD | |
| D835Y | 0.8 |
| FLT3-JM-PM | |
| V592A | 0.7 |
| V579A | 0.8 |
| F594L | 0.9 |
| F590GY591D | 0.7 |
Mutation class . | IC50 PKC412, nM . |
|---|---|
| FLT3-ITD | |
| W51 | 5.0 |
| FLT3-TKD | |
| D835Y | 0.8 |
| FLT3-JM-PM | |
| V592A | 0.7 |
| V579A | 0.8 |
| F594L | 0.9 |
| F590GY591D | 0.7 |
FLT3-WT, FLT3-W51, FLT3-D835Y, and the FLT3-JM-PM mutants FLT3-V592A, FLT3-V579A, FLT3-F594L, and FLT3-F590GY591D expressing Ba/F3 cells were seeded at a density of 4 × 104 cells/mL in the absence or presence of different concentrations of PKC412 (0 to 50 nM) and counted after 72 hours. All cell lines were also cultured in the presence of IL-3 and 50 nM PKC412 to confirm nontoxicity of PKC412 to Ba/F3 cells. The IC50 was calculated from three independent experiments.