Table 1. Proliferation IC50 (nM) of FLT3 TKI against AL mutants.
| FLT3 mutants mut |
Midostaurin | Lestaurtinib | AG1295 | AGS324 | Linifanib | Quizartinib | Sunitinib | Sorafenib | TTT-3002 | R406 | KW2449 | Crenolanib | Ponatinib |
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| FLT3-ITD | 9.3 | 8.6 | 297.9 | 65.3 | 2.4 | 1.2 | 5.4 | 18.5 | <1.0 | 165.6 | 41.0 | 57.0 | <1.0 |
| D835Y | 10.0 | 9.8 | >3000 | >3000 | >100 | >100 | >100 | >2000 | 4.1 | >200 | >200 | 58.0 | 92.0 |
| D835A | 5.0 | 5.0 | 1972.0 | >200 | >200 | >200 | >200 | >200.0 | 1.3 | >200 | 62.0 | 78.1 | 148.2 |
| D835G | 7.9 | 6.0 | 423.0 | 60.1 | 8.6 | 9.0 | 48.1 | 34.5 | <1.0 | 141.0 | 56.0 | 110 | <1.0 |
| D835N | 8.4 | 7.6 | 411.1 | 100 | 10.3 | 7.2 | 46.4 | 31.6 | <1.0 | 153.0 | 58.3 | 80.0 | <1.0 |
| D835L+K | 1.0 | 2.1 | >3000 | >3000 | >200 | >200 | >200 | >200 | 6.7 | >200 | >200 | >1000 | >1000 |
| I836L+D | 5.2 | 2.1 | >3000 | >3000 | >200 | >200 | >200 | >200 | 11.7 | >200 | >200 | 50.0 | <1.0 |
| I836S | 10.2 | 15.0 | >3000 | >200 | >200 | >200 | >200 | 10.2 | 9.0 | >200 | >200 | >1000 | >1000 |
| I836T | 10.0 | 13.4 | >3000 | >3000 | 5.3 | 6.8 | 6.0 | 48.2 | 9.7 | 152.0 | 31.9 | >1000 | >1000 |
| 840G+S | 12.0 | 8.0 | 500.0 | 50.0 | 2.1 | 2.5 | 4.0 | 5.0 | <1.0 | >200 | 35.0 | 83.0 | <1.0 |
| D593D | 2.4 | 8.0 | >3000 | >200 | >200 | >200 | >200 | >200.0 | 2.8 | >200 | >200 | 70.0 | 10.7 |