High quality CAS:936091-26-8 in stock CAS NO.936091-26-8

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).[1] in treated cells the inhibitor blocks downstream cellular signalling (jak-stat) leading to suppression of proliferation and induction of apoptosis.

myelofibrosis is a myeloid malignancy associated with anemia, splenomegaly, and constitutional symptoms. patients with myelofibrosis frequently harbor jak-stat activating mutations that are sensitive to tg101348. phase i trial results focused on safety and efficacy of tg101348 in patients with high- or intermediate-risk primary or post–polycythemia vera/essential thrombocythemia myelofibrosis have been published in 2011.

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