别名:   FGFR-1β (IIIc)/Fc Chimera

•  MDL number  MFCD03456785

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产品名称

Analysis Note

The bioactivity is measured by its ability to inhibit human fibroblast growth factor acidic-dependent proliferation of NR6 cells.

Physical form

Lyophilized from a 0.2 μm filtered solution in phosphate buffered saline.

Biochem/physiol Actions

Studies in genetically modified mice show that the epithelial-stromal interaction mediated by FGFR1 and FGF are responsible for the pathophysiology of prostate cancer. The antitumor property of dovitinib is mediated by the inhibition of FGFR1 signaling in prostate cancer to prevent bone metastasis. In malignant pleural mesothelioma (MPM), FGFR1 mRNA levels are elevated, though the gene is not amplified. FGFR1 autocrine signaling is implicated in the tumorigenesis of MPM, and thus, FGFR1 pathway has potential as a therapeutic target in the same. This gene is amplified in squamous cell lung cancer, head and neck squamous cell cancer (HNSCC) and breast cancer. Expression of FGFR1β on glial cells is thought to promote glial cell growth and malignancy.

General description

FGFR1 (fibroblast growth factor receptor 1) is one of the four variants of FGFR, the ligand of which are the FGF polypeptides. FGFRs are highly conserved in nature, and the variants differ in their intracellular kinase and extracellular ligand-binding domains. It is a receptor tyrosine kinase localized to the human chromosome 8p12. Absence of the α exon leads to the production of FGFR1β isoform, which on glial cells during neoplastic differentiation. This isoform has only two immunoglobulin (Ig) domains unlike FGFR1α, which has three Ig domains. Lack of third Ig domain in this isoform results in FGFR1β having higher affinity for acidic and basic FGFs.

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