A small molecule inhibitor of JAK2 (IC50 = 6 nM) and the related kinases FLT3 (IC50 = 25 nM) and RET (IC50 = 17 nM) with significantly less potent activity against JAK3 (IC50 = 169 nM); inhibits the growth of Ba/F3 cells expressing JAK2V617F or MPLW515L mutations (IC50 = 200 nM)

TG101348 – 5 mg

Brand:
Cayman
CAS:
936091-26-8
Storage:
-20
UN-No:
Non-Hazardous - /

Janus kinases (JAKs) are non-receptor kinases that mediate signaling through cytokine receptors, often to members of the signal transducer and activator of transcription (STAT) family.{20362} JAK2V617F and MPLW515L/K are two known mutations that cause dysregulated JAK/STAT signaling in myeloproliferative disorders. TG101348 is a small molecule inhibitor of JAK2 (IC50 = 6 nM) and the related kinases FLT3 (IC50 = 25 nM) and RET (IC50 = 17 nM) with significantly less potent activity against JAK3 (IC50 = 169 nM).{23418} It can inhibit the growth of Ba/F3 cells expressing JAK2V617F or MPLW515L mutations with an IC50 value of 200 nM.{23418} Phase I clinical trial results that 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.{27682}  

 

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Description

A small molecule inhibitor of JAK2 (IC50 = 6 nM) and the related kinases FLT3 (IC50 = 25 nM) and RET (IC50 = 17 nM) with significantly less potent activity against JAK3 (IC50 = 169 nM); inhibits the growth of Ba/F3 cells expressing JAK2V617F or MPLW515L mutations (IC50 = 200 nM)

Formal name: N-(1,1-dimethylethyl)-3-[[5-methyl-2-[[4-[2-(1-pyrrolidinyl)ethoxy]phenyl]amino]-4-pyrimidinyl]amino]-benzenesulfonamide

Synonyms:  Fedratinib|SAR302503

Molecular weight: 524.7

CAS: 936091-26-8

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|JAK Family||Product Type|Biochemicals|Kinase Inhibitors|Other Receptor Tyrosine Kinases||Product Type|Biochemicals|Kinase Inhibitors|PDGFR Family||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Signaling|Growth Factor Receptor Signaling||Research Area|Cancer|Cell Signaling|JAK/STAT Signaling||Research Area|Cell Biology|Cell Signaling|JAK Signaling

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