OVERVIEW
DOCUMENTS/REFERENCES
Biological Information
Background Information:
Two high affinity VEGF receptors, FLT1 (VEGFR-1, activated by placental growth factor PlGF) and KDR (Flk-1/VEGFR-2, activated by VEGF), have been identified. These receptors can be divided into three structural regions: seven extracellular Ig-like domains that contain the growth factor binding sites, a single polypeptide chain hydrophobic trans-membrane sequence, and intracellular cytoplasmic domains that confer the tyrosine kinase activity required for signal transduction. VEGF-B and VEGF-D homologues bind with high affinity to FLT1 (fms-related tyrosine kinase 1, vascular endothelial growth factor/vascular permeability factor receptor).
Family:
Kinase
Sub Family:
RTK
Class:
Protein Tyrosine
Protein Name:
Flt-1 (VEGFR1)
Uniprot Number:
P17948
Protein Aliases:
vascular endothelial growth factor receptor 1|vascular permeability factor receptor
Gene Name:
FLT1
Gene ID:
2321
Gene Aliases:
FLT|FRT|VEGFR1
Accession Number:
AF063657
Organism:
Human
Construct Details:
783-end recombinant
Assay Information
Assay Type:
Biochemical
Assay Sub Type:
Enzymatic
Functional Mode:
Antagonist
Detection Method:
Radiometric
Measured Response:
Scintillation
Testing Information
Procedure Summary:
Flt1 (h) is incubated with 8 mM MOPS pH 7.0, 0.2 mM EDTA, 250 µM KKKSPGEYVNIEFG, 10 mM MgAcetate and [g- 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:
250 µM KKKSPGEYVNIEFG
Tracer:
33P
ATP Concentration:
[ATP]= 200µM (Km= 505µM )
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
Adverse / Beneficial Action:
Tyrosine kinase FLT1 inhibitors may be useful in the treatment of tumor angiogenesis.
Additional Information
Brand:
LeadHunter
Testing Location:
KP - France - Celle L'Evescault
RELATED SOLUTIONS
Flt-1 (VEGFR1) (FLT1) Human RTK Kinase Enzymatic Radiometric [10 uM ATP] KinaseProfiler LeadHunter Assay - FR
Item: 14-923KP10
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