Fedratinib (SAR302503)

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.