Fedratinib (TG-101348) is a JAK2 inhibitor that is selective, ATP-competitive, and orally active, inhibiting JAK2 and JAK2V617F kinases (IC50=3 nM). Fedratinib induces apoptosis in tumor cells and may be used in myeloproliferative diseases.

IC50 values for TG101348 are determined commercially using the InVitrogen kinase profiling service for a 223 kinase screen that included JAK2 and JAK2V617F or Carna Biosciences for the screen of all Janus kinase family members including JAK1 and Tyk2. ATP concentration is set to approximately the Km value for each kinase

JAK2 (V617F):3 nM (cell free), RET:48 nM (cell free), FLT3:15 nM (cell free), JAK2:3 nM (cell free)

524.678

C27H36N6O3S

CC1=CN=C(NC2=CC=C(OCCN3CCCC3)C=C2)N=C1NC1=CC(=CC=C1)S(=O)(=O)NC(C)(C)C

1.247g/cm3

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