OVERVIEW
DOCUMENTS/REFERENCES
Biological Information
Background Information:
Three high affinity VEGF receptors, Flt-1 (VEGFR-1, activated by placental growth factor PlGF), KDR (Flk-1/VEGFR-2, activated by VEGF), and FLT4 (VEGF3, activated by VEGF-related protein (VRP)), 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. Tissue expression of the FLT4 receptor is found predominantly in lymphatic and microvascular endothelium and some leukemia cell lines, indicating that this receptor may be a role in the regulation of hematopoiesis.
Family:
Kinase
Sub Family:
RTK
Class:
Protein Tyrosine
Protein Name:
FLT4
Uniprot Number:
P35916
Protein Aliases:
Fms-like tyrosine kinase 4|FLT-4|Tyrosine-protein kinase receptor FLT4
Gene Name:
FLT4
Gene ID:
2324
Gene Aliases:
VEGFR3|PCL
Accession Number:
NM_182925
Organism:
Human
Construct Details:
800-end; V1128L; H1146R recombinant
Assay Information
Assay Type:
Biochemical
Assay Sub Type:
Enzymatic
Functional Mode:
Antagonist
Detection Method:
Radiometric
Measured Response:
Scintillation
Testing Information
Procedure Summary:
Flt4 (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= 237.50µM )
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 FLT4 inhibitors may be useful in the treatment of tumor angiogenesis cancer progression and metastasis to regional lymph nodes.
Additional Information
Brand:
LeadHunter
Testing Location:
KP - France - Celle L'Evescault
RELATED SOLUTIONS
FLT4 Human RTK Kinase Enzymatic Radiometric [Km ATP] KinaseProfiler LeadHunter Assay - FR
Item: 14-681KP
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