936091-26-8

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Product Description

Name	N-tert-butyl-3-[[5-methyl-2-[4-(2-pyrrolidin-1-ylethoxy)anilino]pyrimidin-4-yl]amino]benzenesulfonamide
Synonyms	TG 101348；Fedratinib;N-(1,1-Dimethylethyl)-3-[[5-methyl-2-[[4-[2-(1-pyrrolidinyl)ethoxy]phenyl]amino]-4-pyrimidinyl]amino]benzenesulfonamide
Molecular Formula	C₂₇H₃₆N₆O₃S
Molecular Weight	524.68
CAS Number	936091-26-8
purity	≥98%
Storage conditions	Keep in dark place,Inert atmosphere,Store in freezer, under -20°C

Applications：

TG101348 (SAR302503) TG101348 (CAS:936091-26-8) 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). 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 TG101348 (CAS:936091-26-8). Phase I trial results focused on safety and efficacy of TG101348 TG101348 (CAS:936091-26-8) in patients with high- or intermediate-risk primary or post–polycythemia vera/essential thrombocythemia myelofibrosis have been published in 2011.
Compound was originally discovered TargeGen then acquired by Sanofi-Aventis who continues its development under the code SAR302503.

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