Activity of NVP-BSK805 in cellular assays
| Cellular assay | NVP-BSK805, GI50, IC50 (μmol/L) | JAK inhibitor 1, GI50 (μmol/L) |
|---|---|---|
| Ba/F3 JAK2V617F proliferation assay | 0.039 ± 0.023 | ND |
| SET-2 JAK2V617F proliferation assay | 0.051 ± 0.018 | 0.070 ± 0.017 |
| MB-02 JAK2V617F proliferation assay | 0.064 ± 0.017 | 0.022 ± 0.003 |
| UKE-1 JAK2V617F proliferation assay | 0.071 ± 0.002 | 0.104 ± 0.013 |
| MUTZ-8 JAK2V617F proliferation assay | 0.331 ± 0.090 | 0.227 ± 0.047 |
| SET-2 JAK2V617F P-STAT5 Surefire AlphaScreen | 0.140 ± 0.046 | ND |
| HT1080 STAT1-GFP nuclear translocation assay | 0.267 ± 0.015 | 0.180 ± 0.066 |
| MOLM-13 FLT3-ITD proliferation assay | 0.309 ± 0.023 | 0.300 ± 0.060 |
| MV4;11 FLT3-ITD proliferation assay | 0.062 ± 0.022 | 0.333 ± 0.172 |
| CMK JAK3A572V proliferation assay | 2.160 ± 0.167 | 0.431 ± 0.046 |
| K-562 BCR-ABL proliferation assay | 1.471 ± 0.081 | >10 |
NOTE: Where indicated, the pan-JAK inhibitor “JAK inhibitor 1” was assessed for the sake of reference. GI50 (proliferation assays) and IC50 (AlphaScreen and Cellomics NucTrans assay) values represent means of at least two independent experiments ± SD.
Abbreviation: ND, not determined.