Table 2.

Activity of NVP-BSK805 in cellular assays

Cellular assayNVP-BSK805, GI50, IC50 (μmol/L)JAK inhibitor 1, GI50 (μmol/L)
Ba/F3 JAK2V617F proliferation assay0.039 ± 0.023ND
SET-2 JAK2V617F proliferation assay0.051 ± 0.0180.070 ± 0.017
MB-02 JAK2V617F proliferation assay0.064 ± 0.0170.022 ± 0.003
UKE-1 JAK2V617F proliferation assay0.071 ± 0.0020.104 ± 0.013
MUTZ-8 JAK2V617F proliferation assay0.331 ± 0.0900.227 ± 0.047
SET-2 JAK2V617F P-STAT5 Surefire AlphaScreen0.140 ± 0.046ND
HT1080 STAT1-GFP nuclear translocation assay0.267 ± 0.0150.180 ± 0.066
MOLM-13 FLT3-ITD proliferation assay0.309 ± 0.0230.300 ± 0.060
MV4;11 FLT3-ITD proliferation assay0.062 ± 0.0220.333 ± 0.172
CMK JAK3A572V proliferation assay2.160 ± 0.1670.431 ± 0.046
K-562 BCR-ABL proliferation assay1.471 ± 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.