F5055
FGFR1 (FLT2) (399-822), active, GST tagged human
PRECISIO® Kinase, recombinant, expressed in baculovirus infected Sf9 cells, ≥70% (SDS-PAGE), buffered aqueous glycerol solution
Synonym(s):
BFGFR, C-FGR, CD331, CEK, FLG, FLT2, KAL2, N-SAM
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About This Item
NACRES:
NA.32
UNSPSC Code:
51111800
Specific activity:
150-204 nmol/min·mg
Assay:
≥70% (SDS-PAGE)
Recombinant:
expressed in baculovirus infected Sf9 cells
recombinant
expressed in baculovirus infected Sf9 cells
product line
PRECISIO® Kinase
assay
≥70% (SDS-PAGE)
form
buffered aqueous glycerol solution
specific activity
150-204 nmol/min·mg
mol wt
~73 kDa
UniProt accession no.
shipped in
dry ice
storage temp.
−70°C
Quality Level
Gene Information
human ... FGFR1(2260)
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.
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.
Physical form
Supplied in 50 mM Tris-HCl, pH 7.5, with 150 mM NaCl, 0.2 5mM DTT, 0.1 mM EGTA, 0.1 mM EDTA, 0.1 mM PMSF, and 25% glycerol.
Legal Information
PRECISIO is a registered trademark of Merck KGaA, Darmstadt, Germany
Storage Class
10 - Combustible liquids
wgk
WGK 1
flash_point_f
Not applicable
flash_point_c
Not applicable
ppe
Eyeshields, Gloves, multi-purpose combination respirator cartridge (US)
Regulatory Information
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Xinhai Wan et al.
Science translational medicine, 6(252), 252ra122-252ra122 (2014-09-05)
Bone is the most common site of prostate cancer (PCa) progression to a therapy-resistant, lethal phenotype. We found that blockade of fibroblast growth factor receptors (FGFRs) with the receptor tyrosine kinase inhibitor dovitinib has clinical activity in a subset of
X Xu et al.
Cell and tissue research, 296(1), 33-43 (1999-04-13)
Fibroblast growth factor (FGF) receptors constitute a family of four membrane-spanning tyrosine kinases (FGFR1-4) which serve as high-affinity receptors for 17 growth factors (FGF1-17). To study functions of FGF/ FGFR signals in development, mice that carry mutations in each receptor
M Fernanda Amary et al.
Cancer medicine, 3(4), 980-987 (2014-05-28)
Osteosarcoma, the most common primary bone sarcoma, is a genetically complex disease with no widely accepted biomarker to allow stratification of patients for treatment. After a recent report of one osteosarcoma cell line and one tumor exhibiting fibroblastic growth factor
Casper Groth et al.
The International journal of developmental biology, 46(4), 393-400 (2002-07-27)
The vertebrate fibroblast growth factor receptor 1 (FGFR1) is alternatively spliced generating multiple splice variants that are differentially expressed during embryo development and in the adult body. The restricted expression patterns of FGFR1 isoforms, together with differential expression and binding
Lindsay A Marek et al.
Molecular cancer research : MCR, 12(10), 1460-1469 (2014-06-27)
Malignant pleural mesothelioma (MPM) is associated with asbestos exposure and is a cancer that has not been significantly affected by small molecule-based targeted therapeutics. Previously, we demonstrated the existence of functional subsets of lung cancer and head and neck squamous
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