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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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Recifercept
产品货号 : M36832
cas no: 2226238-09-9
Recifercept (TA-46) 是一种可溶性重组成纤维细胞生长因子受体3 (FGFR3) 分子。Recifercept 可作为诱饵/配体陷阱，以减少可与突变 FGFR3 受体结合的成纤维细胞生长因子的数量。Recifercept 可用于软骨发育不全的研究。
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Vofatamab
产品货号 : M36756
cas no: 1312305-12-6
Vofatamab (B-701) 是一种抗 FGFR3 单克隆抗体 (mAb)。Vofatamab 阻断野生型和基因激活受体的激活。Vofatamab 可用于转移性尿路上皮癌 (Muc) 的研究。
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Bemarituzumab
产品货号 : M36659
cas no: 1952272-74-0
Bemarituzumab 是一种针对 FGFR2b (一种 FGF 受体) 的首创的人源化 IgG1 单克隆抗体。Bemarituzumab 阻止成纤维细胞生长因子结合和激活 FGFR2b。Bemarituzumab 具有用于癌症研究的潜力。
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Aprutumab
产品货号 : M36658
cas no: 1634620-63-5
Aprutumab (BAY 1179470) 是一种人源 FGFR2 单克隆抗体，可与 FGFR2 同工型FGFR2-IIIb 和 FGFR2-IIIc 结合。Aprutumab 具有用于实体瘤研究的潜力。
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FGFR2-IN-2
产品货号 : M35560
cas no: 2677709-81-6
FGFR2-IN-2 (Compound 38) 是一种选择性 FGFR2 抑制剂，对 FGFR1、FGFR2 和 FGFR3 的 IC50 分别为 389、29 和 758 nM。
