Table 3. . IC50 (proliferation) and FMS-like tyrosine kinase 3 inhibition of activity.
| Compound | % inhibition of FLT3 activity (500 nM) | IC50 (nM) | |
|---|---|---|---|
| MV4–11 | MOLM14 | ||
| HSN248 (D7) | 73% | 181 ± 6.5 | 180 ± 7.8 |
| HSN178 (D15) | 66% | 144 ± 2.6 | 187 ± 5.5 |
| HSN247 (D6) | 74% | 154 ± 7.1 | 129 ± 8.2 |
| HSM1702 (A15) | 66% | 71 ± 1.1 | 102 ± 11 |
| HSN315 (D28) | 32% | 549 ± 7.4 | 523 ± 6.4 |
| HSN285 | 28% | 721 ± 5.8 | 415 ± 6.9 |
| HSN286 (D30) | 97% | 0.49 ± 0.02 | 0.72 ± 0.02 |
| HSN325 | 33% | 135 ± 5.87 | 456 ± 15 |
| HSN334 | 99% | 1.38 ± 0.1 | 1.61 ± 0.02 |
| HSN353 | 94% | 3.45 ± 0.04 | 1.97 ± 0.1 |
| HSN352 | 93% | 3.09 ± 0.1 | 3.01 ± 0.1 |
| HSN356 | 98% | 0.42 ± 0.02 | 0.62 ± 0.02 |
| Midostaurin | 98%† | 18.5 ± 2.5 | 7.37 ± 0.1 |
†% FLT3 inhibition at 412 nM.
FLT3: FMS-like tyrosine kinase 3.