Ruxolitinib phosphate (INCB-018424 phosphate, INCB18424 phosphate) potent, selective, orally active JAK1/JAK2 inhibitor with IC50 of 3.3/2.8 nM, respectively.
Ruxolitinib displays modest selectivity against Tyk2 (6-fold) and marked selectivity (>130-fold) against JAK3.
Ruxolitinib inhibits IL-6 signaling (IC50=281 nM), and proliferation of JAK2V617F(+) Ba/F3 cells (IC50=127 nM).
Ruxolitinib suppresses erythroid progenitor colony formation from JAK2V617F(+) polycythemia vera patients (IC50=67 nM) in primary cultures.
Ruxolitinib markedly reduces level of inflammatory cytokines, and preferentially eliminates neoplastic cells in a mouse model of JAK2V617F(+) MPN.
