Table 1. Mean IC50 of FF-10101 against FLT3 mutant isoforms as compared to other type I and type II FLT3 inhibitors.
Mean reported from at least 3 biologic experimental replicates. IC50 concentrations for specific drugs have been previously reported where indicated.
| FF-10101 | Gilteritinib1 | Crenolanib2,3 | Quizartinib2,3 | Midostaurin | |
|---|---|---|---|---|---|
|
|
|||||
| FLT3-ITD | 1.8 | 1.8 | 11.2 | 0.4 | 5.8 |
| FLT3-ITD/F691L | 14.5 | 25.4 | 55.4 | 151.1 | 6.2 |
| FLT3-ITD/D698N | 5.1 | 31.5 | 85.3 | 0.6 | 65.3 |
| FLT3-ITD/Y693C | 116.1 | 27.9 | 143.0 | 2 2 | 171.7 |
| FLT3-ITD/Y693N | 25.9 | 23.8 | 129.3 | 1.8 | 213.3 |
| FLT3-ITD/G697S | 22.3 | 117.8 | 146.8 | 6.2 | 169.6 |
| FLT3-ITD/K429E | 1.1 | 6.0 | 26.1 | 0.7 | 20.3 |
| FLT3-ITD/N676K | 1.9 | 3.6 | 27.8 | 1.8 | 33.8 |
| FLT3-ITD/D835V | 4.4 | 3.5 | 13.1 | 176.7 | 4.7 |
| FLT3-ITD/D835Y | 11,1 | 1.1 | 13,9 | 56.7 | 6.8 |
| FLT3-ITD/D835H | 8.5 | 1.1 | 12.4 | 14.0 | 3.9 |
| FLT3-ITD/D835F | 13.0 | 1.2 | 16.5 | 457.0 | 5.3 |
| FLT3-ITD/D835I | 7.1 | 0.9 | 17.3 | 222.7 | 5.2 |
| FLT3-ITD/D835del | 6.0 | 4.2 | 184 | 99.3 | 5.3 |
| FLT3-ITD/D835A | 6.5 | 1.3 | 17.5 | 3 2 | 5.0 |
| FLT3-ITD/D835E | 11.2 | 1.4 | 17.4 | 1.8 | 5.8 |
| FLT3-ITD/D835G | 6.3 | 2.3 | 18.2 | 3.0 | 4.6 |
| FLT3-ITD/D835N | 4.7 | 0.9 | 16.8 | 2.1 | 5 8 |
| FLT3-ITD/F691L/D835V | 76.8 | 17.8 | 62.5 | ||
| FLT3-ITD/D698N/D835V | 24.7 | 31.1 | 68.1 | ||
| FLT3-ITD/Y693C/D835V | 399.9 | 34.2 | 156.3 | ||
| FLT3-ITD/C695S | 316.6 | ||||
| FLT3-ITD/C681S | 6.7 | ||||
| FLT3-ITD/C790S | 3.3 | ||||
| FLT3-ITD/C807S | 14.2 | ||||
| FLT3-ITD/C828S | 11.1 | ||||
| FLT3-ITD/C694S | 14.2 | ||||
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Tarver TC, et al. Blood Adv. 2020 Feb 11;4(3):514–524.
2.
Smith CC, et al. Proc Natl Acad Sci U S A. 2014 Apr 8;111(14):5319–24.
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Smith CC, et al. Leukemia. 2015 Dec;29(12):2390–2.