Table 2.
GZD824 inhibits proliferation in Ba/F3 cells expressing FLT3 and mutant isoforms
| IC50 (nM) | Midostaurin |
Gilteritinib (ASP2215) | Quizartinib |
GZD824 |
|---|---|---|---|---|
| (PKC412) | (AC220) | |||
| BaF3-Tel-FLT3-ITD | 21.8 | 5 | 2 | 1.8 |
| BaF3-tel-FLT3 | 14.4 | 57 | 3.1 | 2.3 |
| BaF3-FLT3-MOLM-ITD | 4 | 3.1 | 0.8 | 0.8 |
| BaF3-FLT3-ITD-D835N | 6.5 | 3.5 | 1.6 | 3 |
| BaF3-FLT3-ITD-Y842H | 1.3 | 1.5 | 5.3 | 3.2 |
| BaF3-FLT3-ITD-Y842R | 1.6 | 2.1 | 7.2 | 4.2 |
| BaF3-tel-FLT3-D835Y | 1 | 2.5 | 2.4 | 5.7 |
| BaF3-FLT3-ITD-D835G | 5.8 | 3.8 | 4.3 | 7.8 |
| BaF3-FLT3-ITD-D835A | 5.8 | 1.9 | 3.1 | 9.3 |
| BaF3-FLT3-ITD-N676D | 62.4 | 9.6 | 8.3 | 7.2 |
| BaF3-FLT3-ITD-F691I | 41.9 | 32.8 | 95 | 1.4 |
| BaF3-FLT3-ITD-G697R | 116.3 | 307 | 22.8 | 9.4 |
| BaF3-FLT3-D835H | 6.6 | 3.4 | 4 | 17.6 |
| BaF3-FLT3-D835V | 3.3 | 3.7 | 40.2 | 34.7 |
| BaF3-FLT3-ITD-D835Y | 6.4 | 2.9 | 35.5 | 35.7 |
| BaF3-FLT3-ITD-D835V | 3.8 | 1.6 | 125.6 | 49.9 |
| BaF3-FLT3-ITD-D835I | 3.5 | 1.6 | 182.8 | 58.5 |
| BaF3-tel-FLT3-R834Q | 63.1 | 252.1 | >1000 | 76.2 |
| BaF3-tel-FLT3-K663Q | 102.1 | 389.7 | >1000 | 853.3 |
The anti-proliferative activities of compounds evaluated with a CCK-8 assay.