BLU-554 (Synonyms: BLU-554) |
| Catalog No.GC19075 |
BLU-554(BLU-554)는 IC50이 5 nM인 강력하고 고도로 선택적인 경구 활성 섬유아세포 성장 인자 수용체 4(FGFR4) 억제제입니다. BLU-554는 FGFR4 신호 전달에 의존하는 간세포 암종(HCC) 모델에서 상당한 항종양 활성을 가지고 있습니다.
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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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