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Description: Fedratinib (formerly SAR302503 or TG101348; brand name Inrebic) is a novel, potent, selective, orally bioavailable, small-molecule and ATP-competitive inhibitor of janus kinase 2 (JAK2) with an IC50 of 3 nM. Fedratinib was approved by FDA in 2019 as an anticancer drug for the treatment of myeloproliferative diseases including myelofibrosis. The selectivity of TG101348 for JAK2 is 35- and 334-fold stronger than that for JAK3 and JAK1 respectively. TG10348 is capable of inducing apoptosis in HEL cells as well BaF/3 cells harboring JAK2V617 mutation and inhibiting hematopoietic progenitor colony formation and erythroid engraftment in samples from polycythemia vera (PV) patients.
References:Cancer Cell. 2008 Apr; 13(4):311-20; Cancer Cell. 2008 Apr; 13(4):321-30; Leukemia. 2010 Jul; 24(7):1378-80.
Related CAS: 1374744-69-0 (TG101348 dihydrochloride hydrate); 936091-26-8 (free base)
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