Description
A potent, selective, orally active JAK1/JAK2 inhibitor with IC50 of 3.3/2.8nM, respectively; displays modest selectivity against Tyk2 (6-fold) and marked selectivity (>130-fold) against JAK3; inhibits IL-6 signaling (IC50=281nM), and proliferation of JAK2V617F (+) Ba/F3 cells (IC50=127nM); suppresses erythroid progenitor colony formation from JAK2V617F (+) polycythemia vera patients (IC50=67nM) in primary cultures; markedly reduces level of inflammatory cytokines, and preferentially eliminates neoplastic cells in a mouse model of JAK2V617F (+) MPN. Bone Cancer Approved