OVERVIEW
DOCUMENTS/REFERENCES
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. FGR3 (FGFR-3, Fibroblast growth factor receptor 3, EC 2.7.1.112) is expressed mainly in bone, central nervous system and tumors. Inhibition of FGR3 may be useful in the treatment of dwarfism as well as some tumors.
Family:
Kinase
Sub Family:
RTK
Class:
Protein Tyrosine
Protein Name:
FGFR3
Uniprot Number:
P22607
Protein Aliases:
CD antigen CD333
Gene Name:
FGFR3
Gene ID:
2261
Gene Aliases:
CEK2|JTK4|CD333
Accession Number:
M58051
Organism:
Human
Construct Details:
447-761 recombinant
Assay Information
Assay Type:
Biochemical
Assay Sub Type:
Enzymatic
Functional Mode:
Antagonist
Detection Method:
Radiometric
Measured Response:
Scintillation
Testing Information
Procedure Summary:
FGFR3 (h) is incubated with 8 mM MOPS pH 7.0, 0.2 mM EDTA, 0.1 mg/mL poly(Glu, Tyr) 4:1, 10 mM MnCl2, 10 mM MgAcetate and [gamma-33P]-ATP (specific activity and concentration as required). The reaction is initiated by the addition of the Mg/ATP mix. After incubation for 40 minutes at room temperature, the reaction is stopped by the addition of phosphoric acid to a concentration of 0.5%. An aliquot of the reaction is then spotted onto a filter and washed four times for 4 minutes in 0.425% phosphoric acid and once in methanol prior to drying and scintillation counting.
Substrate:
0.1 mg/mL poly (Glu,Tyr)
Tracer:
33P
ATP Concentration:
[ATP]= 10µM (Km= 28µM )
Incubation:
40 min at Room temperature
Control Inhibitor:
Staurosporine
Test Sample Requirements:
Please provide compounds dissolved in 100% DMSO (PBS or HBSS prohibited).
Stock solution should be ≥50× the final assay concentration (a 10 mM stock is also acceptable).
Required volume:
– <60 kinase assays: 120 µL of 50× stock
– ≥60 assays: 420 µL of 50× stock
If you supply 10 mM stocks or powder (pre-weighed), we will apply the appropriate conversion.
For batches of ~50 compounds supplied as solids, the TAT will be extended.
Minimum Order Quantity:
2
Turnaround Time
Standard:
6 Business Days
Service Scheduling Note:
Assay is run on a weekly schedule beginning on Friday. Compounds and purchase order must be received on or before 13:00 CET Thursday for the order to be included on the service run that begins on Friday of the same week.
Reference Compound Data
Clinical Relevance
Therapeutic Area:
Oncology/Immuno-Oncology
Additional Information
Brand:
LeadHunter
Testing Location:
KP - France - Celle L'Evescault
RELATED SOLUTIONS
FGFR3 Human RTK Kinase Enzymatic Radiometric [Km ATP] KinaseProfiler LeadHunter Assay - FR
Item: 14-464KP
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