Biological Information
Background Information:
Fibroblast growth factor (FGF) superfamily consists of 23 members, all of which contain a conserved 120 amino acid (aa) core region that contains six identical, interspersed amino acids. Based on the pI factor, two main groups of FGF are named: acidic FGF (aFGF) and basic FGF (bFGF). The superfamily members act extracellularly through four tyrosine kinase FGF receptors (FGR1 through FGR4), with multiple specificities noted for almost all FGFs. Biological binding of aFGF to its receptors will result in phosphorylation of the receptor and non-receptor proteins and generate its function. FGR2 (FGFR-2, Fibroblast growth factor receptor 2, Keratinocyte growth factor receptor 2, EC 2.7.1.112) is expressed mainly in bone, central nervous system, smooth muscle and tumors. Inhibition of FGR2 may inhibit cranial development and arterial repair as well as facilitate formation and proliferation of some tumors (e.g., prostate, thyroid).
Family:
Kinase
Sub Family:
RTK
Class:
Protein Tyrosine
Protein Name:
FGFR2
Uniprot Number:
P21802
Protein Aliases:
Crouzon syndrome|Pfeiffer syndrome
Gene Name:
FGFR2
Gene ID:
2263
Gene Aliases:
CEK3|TK14|TK25|ECT1|K-SAM|CD332|BEK|KGFR|KSAM
Accession Number:
NM_022976
Organism:
Human
Construct Details:
Fragment (456-770), Recombinant
Assay Information
Assay Type:
Biochemical
Assay Sub Type:
Enzymatic
Functional Mode:
Antagonist
Detection Method:
Radiometry
Measured Response:
Scintillation
Testing Information
Procedure Summary:
Human recombinant protein kinase FGFR2 expressed in insect Sf21 cells is used. Test compound and/or vehicle is preincubated with 0.1 U/ml enzyme‡ in modified HEPES buffer pH 7.4 for 15 minutes at 37°C. The reaction is initiated by addition of 200 μg/ml poly(Glu:Tyr), 10 μM ATP and 0.25 μCi [γ32P]ATP for another 30 minute incubation period and terminated by further addition of 3% H3PO4. An aliquot is removed and counted to determine the amount of [32P]Poly(Glu:Tyr) formed. Compounds are screened at 10 μM.
Substrate:
200 µg/ml Poly(Glu:Tyr)
ATP Concentration:
10 uM
Incubation:
30 min at 37°C
Control Inhibitor:
Staurosporine
Criteria For Significance:
≥ 50% of max stimulation or inhibition
Test Concentration / Dose:
Suggested concentration for initial testing is 10 uM
Test Sample Requirements:
Minimum for 1) Screen: 25 μl of 10 mM stock -OR- 1 mg (pre-weighed). 2) Dose Response: 60 μl of 10 mM stock -OR- 1 mg (pre-weighed).
Minimum Order Quantity:
2
Turnaround Time
Standard:
15 Business Days
Reference Compound Data
Clinical Relevance
Therapeutic Area:
Oncology/Immuno-Oncology
Additional Information
Brand:
LeadHunter
Testing Location:
Taiwan - Taipei
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