Kinase selectivity profile of FF-10101
| Kinase . | IC50, nM . | Margin of selectivity . |
|---|---|---|
| FLT3 | 0.20 | 1.0 |
| FLT3 (D835Y) | 0.16 | 0.80 |
| FMS | 0.94 | 4.7 |
| KIT | 2.0 | 10 |
| MINK | 6.8 | 34 |
| KHS1 | 9.1 | 46 |
| KIT (T670I) | 11 | 55 |
| FGR | 12 | 60 |
| IRAK1 | 13 | 65 |
| MELK | 16 | 80 |
| HGK | 17 | 85 |
| Kinase . | IC50, nM . | Margin of selectivity . |
|---|---|---|
| FLT3 | 0.20 | 1.0 |
| FLT3 (D835Y) | 0.16 | 0.80 |
| FMS | 0.94 | 4.7 |
| KIT | 2.0 | 10 |
| MINK | 6.8 | 34 |
| KHS1 | 9.1 | 46 |
| KIT (T670I) | 11 | 55 |
| FGR | 12 | 60 |
| IRAK1 | 13 | 65 |
| MELK | 16 | 80 |
| HGK | 17 | 85 |
Kinase inhibitory activity of FF-10101 was evaluated against 216 kinases. Each enzyme was incubated with FF-10101 dilutions in the presence of ATP at 28°C for 90 minutes. Percent inhibition of enzyme activity was determined, and IC50 values were calculated in accordance with the manufacturer’s protocol. Kinases with IC50 values of less than 20 nM are listed.