Enzymatic and functional potency of INCB018424
| . | IC50, nM (mean ± SD) . | N . |
|---|---|---|
| Enzyme assays | ||
| JAK1 | 3.3 ± 1.2 | 7 |
| JAK2 | 2.8 ± 1.2 | 8 |
| JAK3 | 428 ± 243 | 5 |
| Tyk2 | 19 ± 3.2 | 8 |
| CHK2 | > 1000* | 7 |
| cMET | > 10 000* | 1 |
| Whole blood assays | ||
| IL-6 stimulation | 282 ± 54 | 6 |
| TPO stimulation | 281 ± 62 | 4 |
| . | IC50, nM (mean ± SD) . | N . |
|---|---|---|
| Enzyme assays | ||
| JAK1 | 3.3 ± 1.2 | 7 |
| JAK2 | 2.8 ± 1.2 | 8 |
| JAK3 | 428 ± 243 | 5 |
| Tyk2 | 19 ± 3.2 | 8 |
| CHK2 | > 1000* | 7 |
| cMET | > 10 000* | 1 |
| Whole blood assays | ||
| IL-6 stimulation | 282 ± 54 | 6 |
| TPO stimulation | 281 ± 62 | 4 |
Highest concentration evaluated.
SD indicates standard deviation; IL, interleukin; and TPO, thrombopoietin.