NVP-BSK805 dihydrochloride is a potent, selective and ATP-competitive inhibitor of JAK2 (V617F) and wt JAK2 (IC50=0.5 nM).
NVP-BSK805 displays >20-fold selectivity towards JAK1, JAK3, TYK2 and excellent selectivity in broader kinase profiling.
NVP-BSK805 blunts constitutive STAT5 phosphorylation in JAK2(V617F)-bearing cells.
NVP-BSK805 exhibits good oral bioavailability and a long half-life.
