Discovery and evaluation of ZT55 a novel highly-selective tyrosine kinase inhibitor of JAK2V617F against myeloproliferative neoplasms

摘要

BackgroundThe JAK2-STAT signaling pathway plays a critical role in myeloproliferative neoplasms (MPN). An activating mutation in JAK2 (V617F) is present in ~ 95% of polycythemia vera, essential thrombocythemia, and primary myelofibrosis cases. This study aims to explore the selective JAK2^V617F inhibitor, evaluate the efficacy and possible mechanism of ZT55 on MPN.