Fedratinib, also known as TG101348 and SAR302503, is a JAK2 inhibitor, is also an orally bioavailable, small-molecule, ATP-competitive inhibitor of Janus-associated kinase 2 (JAK2) with potential antineoplastic activity. JAK2 inhibitor TG101348 competes with JAK2 as well as the mutated form AK2V617F for ATP binding, which may result in inhibition of JAK2 activation, inhibition of the JAK-STAT signaling pathway, and the induction of tumor cell apoptosis. JAK2 is the most common mutated gene in bcr-abl-negative myeloproliferative disorders (MPDs); the mutated form JAK2V617F has a valine-to-phenylalanine modification at position 617 and plays a key role in tumor cell proliferation and survival.
Tefferi, Ayalew. N-tert-butyl-3-[(5-methyl-2-{[4-(2-pyrrolidin-1-ylethoxy)phenyl]amino}pyrimidin-4-yl)amino]benzenesulfonamide for treating myelofibrosis. Assignee TargeGen, Inc., USA. WO 2012060847. (2012).
Noronha, Glenn; Mak, Chi Ching; Cao, Jianguo; Renick, Joel; McPherson, Andrew; Zeng, Binqi; Pathak, Ved P.; Lohse, Daniel L.; Hood, John D.; Soll, Richard M. Preparation of pyrimidine derivatives as JAK kinases inhibitors. Assignee TargeGen, Inc., USA. US 20110212077. (2011).
