TG101348
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936091-26-8
≥98%
A crystalline solid
C27H36N6O3S
524.7
n-(1,1-dimethylethyl)-3-[[5-methyl-2-[[4-[2-(1-pyrrolidinyl)ethoxy]phenyl]amino]-4-pyrimidinyl]amino]-benzenesulfonamide, fedratinib, sar302503
A JAK2 inhibitor (IC50 = 3 nM for wild-type and JAK2V617F enzymes); is 35-, 334-, and 135-fold selective for JAK2 over JAK1, JAK3, and TYK2, respectively; selective for JAK2 over a panel of 34 kinases at 500 nM; inhibits FLT3 and RET (IC50s = 15 and 48 nM, respectively); reduces the proliferation of HEL cells as well as Ba/F3 murine cells expressing JAK2V617F (IC50s = 305 and 270 nM, respectively); inhibits the differentiation of hematopoietic stem cells and myeloid progenitor cells isolated from patients with polycythemia vera at 300 nM; improves survival and reduces spleen weight in a syngeneic mouse model of polycythemia vera induced by transplantation of Jak2V617F-expressing whole bone marrow at 60 and 120 mg/kg
