Inhibitory activity of crenolanib against different FLT3 TKD mutations
| Cell line . | Crenolanib . | Quizartinib . | Fold difference . |
|---|---|---|---|
| IC50 pFLT3 (nM) . | IC50 pFLT3 (nM) . | ||
| Ba/F3 ITD | 1.3 | 1.7 | 1.2 |
| Ba/F3 ITD/D835Y | 8.7 | 93.1 | 10.7 |
| Ba/F3 WT D835Y | 6.9 | 33.7 | 4.9 |
| Ba/F3 WT D835F | 6.5 | 72.7 | 11.2 |
| Ba/F3 WT D835H | 19.8 | 20.0 | — |
| Ba/F3 WT D835N | 4.3 | 2.3 | 0.5 |
| Ba/F3 WT D835V | 2.3 | 63.7 | 27.4 |
| Ba/F3 ITD/F691L | 67.8 | 36.4 | 0.5 |
| Cell line . | Crenolanib . | Quizartinib . | Fold difference . |
|---|---|---|---|
| IC50 pFLT3 (nM) . | IC50 pFLT3 (nM) . | ||
| Ba/F3 ITD | 1.3 | 1.7 | 1.2 |
| Ba/F3 ITD/D835Y | 8.7 | 93.1 | 10.7 |
| Ba/F3 WT D835Y | 6.9 | 33.7 | 4.9 |
| Ba/F3 WT D835F | 6.5 | 72.7 | 11.2 |
| Ba/F3 WT D835H | 19.8 | 20.0 | — |
| Ba/F3 WT D835N | 4.3 | 2.3 | 0.5 |
| Ba/F3 WT D835V | 2.3 | 63.7 | 27.4 |
| Ba/F3 ITD/F691L | 67.8 | 36.4 | 0.5 |
Ba/F3 cell lines were treated with quizartinib or crenolanib for 1 hour and then cells were lysed, immunoprecipitated for FLT3, and analyzed by immunoblotting for phospho- and total FLT3. Densitometry analysis was performed using Quantity One software (version 4.5.0). IC50s were calculated by regression analysis after linear conversion (Calcusyn software).