Table 1. Antiproliferative activities of NS-018 and other JAK inhibitors in Ba/F3 cells.
| Compound | Target kinase | Proliferation IC50 (nM) | Selectivity | Interaction with Gly993 | ||
|---|---|---|---|---|---|---|
| |
|
Ba/F3-JAK2WT (+IL-3) |
Ba/F3-JAK2V617F |
V617F/WT |
CH···O |
Water mediated |
| NS-018 | JAK2, Src | 2000 | 470 | 4.3 | Yes | Yes |
| AZD1480 | JAK1/2 | 2300 | 1000 | 2.3 | Yes | No |
| CP-690,550 (tofacitinib) | JAK1/2/3 | 2200 | 760 | 2.9 | No | No |
| INCB018424 (ruxolitinib) | JAK1/2 | 630 | 310 | 2.0 | ||
| CYT387 (momelotinib) | JAK1/2 | 4300 | 2400 | 1.8 | ||
| TG101209 | JAK2 | 850 | 550 | 1.5 | ||
| TG101348 (fedratinib) | JAK2 | 1000 | 650 | 1.5 | ||
| AT9283 | JAK2/3, Aurora | 48 | 48 | 1.0 | No | No |
Abbreviation: JAK, Janus kinase 2.