FGFR Human RTK Kinase Enzymatic Radiometric LeadHunter Assay [10 μM ATP] - TW
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 (FGFR1 through FGFR4), 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. Overexpression and amplification of the fibroblast growth factor receptor-1 (FGFR-1), a prototypic receptor tyrosine kinase, have been found in tumor samples from human pancreas, breast, brain, prostate, thyroid gland, and salivary gland.
Family:
Kinase
Sub Family:
RTK
Class:
Protein Tyrosine
Protein Name:
FGFR1
Uniprot Number:
P11362
Protein Aliases:
Pfeiffer syndrome
Gene Name:
FGFR1
Gene ID:
2260
Gene Aliases:
H2|H3|H4|H5|CEK|FLG|BFGFR|N-SAM|CD331
Accession Number:
NM_001174063
Organism:
Human
Construct Details:
Fragment (456-765), 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 FGFR1 expressed in insect Sf21 cells is used. Test compound and/or vehicle is preincubated with 70 mU/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
Adverse / Beneficial Action:
Inhibition of FGFR1 may inhibit cranial development and arterial repair as well as facilitate formation and proliferation of some tumors (e.g., prostate, thyroid).
Additional Information
Brand:
LeadHunter
Testing Location:
Taiwan - Taipei
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Item: PP90
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