FGFR1 (V561M) Human RTK Kinase Enzymatic Radiometric [10 uM ATP] KinaseProfiler LeadHunter Assay - FR

Item: 14-734KP10

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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_000604

Organism:

Human

Construct Details:

456-765; V561M recombinant

Assay Information

Assay Type:

Biochemical

Assay Sub Type:

Enzymatic

Functional Mode:

Antagonist

Detection Method:

Radiometric

Measured Response:

Scintillation

Testing Information

Procedure Summary:

FGFR1 (V561M) (h) is incubated with 8 mM MOPS pH 7.0, 0.2 mM EDTA, 500 µM GGEEEEYFELVKKKK, 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:

500 µM GGEEEEYFELVKKKK

Tracer:

33P

ATP Concentration:

[ATP]= 10µM (Km= 45µM )

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:

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

PubChem ID

122130844

Name

Staurosporine

Measurement

0.22nM - IC50

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:

KP - France - Celle L'Evescault