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FGFR
The fibroblast growth factor/fibroblast growth factor receptor (FGF/FGFR) is a receptor tyrosine kinase (RTK) signaling pathway that fundamentally regulates embryogenesis, angiogenesis, tissue homeostasis, and wound repair. The FGF family contains 22 known ligands and FGFs interact with the extracellular matrix as well as the cell surface via stabilization by heparan sulphate proteoglycans (HSPGs). The communications of FGFs with HSPGs has been shown to be essential for FGF signal transduction. The FGFR receptors (1-4) can become activated by mutation, translocation, or gene amplification. An increase in circulating FGF ligands can also cause activation. Downstream signaling can trigger the mitogen activated protein kinase (MAPK) pathway, the phosphoinositide-3-kinase (PI3K/Akt) pathway, the phosphorylation of the signal transducer and activator of transcription (STAT), and the PLCγ activation of the DAG-PKC and IP3-Ca2+ cascade resulting in DNA transcription. Negative feedback loops can attenuate the signaling cascade at varying levels. The FGFR signaling pathway represents a major target for cancer therapeutics as it plays a crucial role in tumor proliferation, angiogenesis, migration, and survival.
References
1.Chae YK, et al. Oncotarget. 2017;8(9):16052–16074.
References
1.Chae YK, et al. Oncotarget. 2017;8(9):16052–16074.
Angiogenesis
FGFR
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FGFR1/DDR2 inhibitor 1
产品货号 : M24051
cas no: 2308497-58-5
FGFR1/DDR2抑制剂1是discoindin结构域受体2 (DDR2)和成纤维细胞生长因子受体1 (FGFR1)的抑制剂，对FGFR1、KG-1和DDR2的IC50值分别为31.1 nM、108.4 nM和3.2 nM。
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SU4984
产品货号 : M23849
cas no: 186610-89-9
SU4984 是一种细胞渗透性、ATP 竞争性和可逆性成纤维细胞生长因子受体 1 (FGFR1) 抑制剂。
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FGFR4-IN-1
产品货号 : M23769
cas no: 1708971-72-5
FGFR4-IN-1 是一种有效的 FGFR4 抑制剂 (IC50: 0.7 nM)。
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Lucitanib
产品货号 : M23262
cas no: 1058137-23-7
Lucitanib 是一种新型 VEGFR 和 FGFR 抑制剂。
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PRN1371
产品货号 : M22475
cas no: 1802929-43-6
PRN1371 是一种特异性、有效的 FGFR1-4 和 CSF1R 抑制剂（对于 FGFR1/2/3/4 和 CSF1R，IC50：0.6/1.3/4.1/19.3/8.1 nM）。
