REVIEW WP1066 inhibits JAK2 and its downstream signal transducer and activator of transcription-3 (STAT3), signal transducer and activator of transcription-5 (STAT5), and extracellular signal-regulated kinase-1/2 pathways (ERKs) in a dose- and time-dependent manner. The compound has also been show to suppress proliferation and induce apoptosis in erythroid human cells carrying the JAK2 V617F mutation.
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Ferrajoli, Alessandra; Faderl, Stefan; Van, Quin; Koch, Patricia; Harris, David; Liu, Zhiming; Hazan-Halevy, Inbal; Wang, Yongtao; Kantarjian, Hagop M.; Priebe, Waldemar; et al WP1066 Disrupts Janus Kinase-2 and Induces Caspase-Dependent Apoptosis in Acute Myelogenous Leukemia Cells Cancer Research (2007), 67(23), 11291-11299.
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Verstovsek S, Manshouri T, Quintás-Cardama A, Harris D, Cortes J, Giles FJ, Kantarjian H, Priebe W, Estrov Z WP1066, a novel JAK2 inhibitor, suppresses proliferation and induces apoptosis in erythroid human cells carrying the JAK2 V617F mutation. Clin Cancer Res. 2008 Feb 1;14(3):788-96.
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