Tags: Chemical Compound, Chemical Substance.

TG101348 (SAR302503) is an orally available inhibitor of Janus kinase 2 (JAK-2) developed for the treatment of patients with myeloproliferative diseases including myelofibrosis. TG101348 acts as a competitive inhibitor of protein kinase JAK-2 with IC50=6 nM; related kinases FLT3 and RET are also sensitive with IC50=25 nM and IC50=17 nM respectively. Significantly less activity was observed against other tyrosine kinases including JAK3 (IC50=169 nM).

TG_101348.svg
IUPAC name
N-tert-Butyl-3-5-methyl-2-[4-(2-pyrrolidin-1-yl-ethoxy)-phenylamino]-pyrimidin-4-ylamino-benzenesulfonamide

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