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- TG101348 abstract "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). 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.Compound was originally discovered TargeGen then acquired by Sanofi-Aventis who continues its development under the code SAR302503.".
- TG101348 iupacName "N-tert-Butyl-3-{5-methyl-2-[4-(2-pyrrolidin-1-yl-ethoxy)-phenylamino]-pyrimidin-4-ylamino}-benzenesulfonamide".
- TG101348 thumbnail TG_101348.svg?width=300.
- TG101348 wikiPageExternalLink 15406_RD_Portfolio_Phase_I-II_2011-09-06.pdf.
- TG101348 wikiPageID "33860916".
- TG101348 wikiPageLength "3599".
- TG101348 wikiPageOutDegree "9".
- TG101348 wikiPageRevisionID "679068549".
- TG101348 wikiPageWikiLink Category:Protein_kinase_inhibitors.
- TG101348 wikiPageWikiLink Category:Pyrimidines.
- TG101348 wikiPageWikiLink Category:Sulfonamides.
- TG101348 wikiPageWikiLink JAK-STAT_signaling_pathway.
- TG101348 wikiPageWikiLink Janus_kinase_inhibitor.
- TG101348 wikiPageWikiLink Myelofibrosis.
- TG101348 wikiPageWikiLink Protein_kinase.
- TG101348 wikiPageWikiLink Sanofi.
- TG101348 wikiPageWikiLinkText "TG101348".
- TG101348 imagefile "TG 101348.svg".
- TG101348 imagesize "200".
- TG101348 iupacname "N-tert-Butyl-3-{5-methyl-2-[4--phenylamino]-pyrimidin-4-ylamino}-benzenesulfonamide".
- TG101348 othernames "302503.0".
- TG101348 wikiPageUsesTemplate Template:Cascite.
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- TG101348 wikiPageUsesTemplate Template:Chembox_Hazards.
- TG101348 wikiPageUsesTemplate Template:Chembox_Identifiers.
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- TG101348 subject Category:Protein_kinase_inhibitors.
- TG101348 subject Category:Pyrimidines.
- TG101348 subject Category:Sulfonamides.
- TG101348 type ChemicalCompound.
- TG101348 type ChemicalSubstance.
- TG101348 type Amide.
- TG101348 type Chemical.
- TG101348 type Diazine.
- TG101348 type Inhibitor.
- TG101348 type Sulfonamide.
- TG101348 type ChemicalObject.
- TG101348 type Thing.
- TG101348 type Q11173.
- TG101348 comment "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).".
- TG101348 label "TG101348".
- TG101348 sameAs Q7670147.
- TG101348 sameAs m.0hnb6wz.
- TG101348 sameAs TG101348.
- TG101348 sameAs TG101348.
- TG101348 sameAs Q7670147.
- TG101348 wasDerivedFrom TG101348?oldid=679068549.
- TG101348 depiction TG_101348.svg.
- TG101348 isPrimaryTopicOf TG101348.