BLU-554 (Synonyms: BLU-554) |
| Catalog No.GC19075 |
Le BLU-554 (BLU-554) est un inhibiteur puissant, hautement sélectif et actif par voie orale du récepteur 4 du facteur de croissance des fibroblastes (FGFR4) avec une IC50 de 5 nM. Le BLU-554 a une activité anti-tumorale significative dans les modèles de carcinome hépatocellulaire (HCC) qui dépendent de la signalisation FGFR4.
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Cas No.: 1707289-21-1
Sample solution is provided at 25 µL, 10mM.
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BLU-554 is a potent fibroblast growth factor receptor 4 (FGFR4) inhibitor.
Fibroblast growth factor receptor 4 (FGFR-4) is a protein that in humans is encoded by the FGFR-4 gene. This protein is a member of the fibroblast growth factor receptor family, where amino acid sequence was highly conserved between members throughout evolution. FGFR family members 1-4 differ from one another in their ligand affinities and tissue distribution. A full-length representative protein consists of an extracellular region composed of three immunoglobulin-like domains, a single hydrophobic membrane-spanning segment and a cytoplasmic tyrosine kinase domain. The extracellular portion of the protein interacts with fibroblast growth factors, setting in motion a cascade of downstream signals, ultimately influencing mitogenesis and differentiation. The genomic organization of the FGFR-4 gene encompasses 18 exons. Although alternative splicing has been observed, there is no evidence that the C-terminal half of the Iglll domain of this protein varies between three alternate forms, as indicated for FGFR 1-3[1].
References:
[1]. Neil Bifulco, et al. Inhibitors of the fibroblast growth factor receptor. PCT Int. Appl. (2015), WO 2015061572 A1 20150430.
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