Table 3. Comparison of LY2784544 with four other clinical JAK2 inhibitors in suppressing JAK2V617F or IL-3-wild-JAK2-mediated STAT5 activation and cell proliferation in Ba/F3 cells.
| Clinical JAK2 inhibitors | pSTAT5 AlphaScreen assay | Cell proliferation assaya | ||
|---|---|---|---|---|
| |
V617F IC50±s.d., nℳ |
WT+IL-3 IC50±s.d., nℳ |
V617F IC50±s.d., nℳ |
WT+IL-3 IC50±s.d., nℳ |
| LY2784544 | 20±4 (n=3) | 1183±860 (n=3) | 55±4 (n=2) | 1309±402 (n=2) |
| AZD1480 | 19±13 (n=3) | 181±132 (n=3) | 43±1 (n=2) | 406±172 (n=2) |
| SAR302503 | 102±36 (n=3) | 1105±460 (n=3) | — | — |
| Ruxolitinib | 24±11 (n=3) | 121±59 (n=3) | 40±6 (n=2) | 331±74 (n=2) |
| CYT387 | 200±12 (n=3) | 2236±1248 (n=2) | — | — |
Abbreviations: IC50, half maximal inhibitory concentration; JAK, janus kinase; n, number of experiments; IL, interleukin; s.d., standard deviation; STAT5, signal transducer and activator of transcription 5; WT, wild-type.
a
Ruxolitinib and AZD1480 were tested in proliferation assays because they are dual inhibitors of JAK1/JAK2.