Flt-1 (VEGFR1) Human RTK Kinase Enzymatic Radiometric LeadHunter Assay [10 μM ATP] - TW
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:
NM_002019
Organism:
Human
Construct Details:
Fragment (783-end), 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 Flt-1 expressed in insect Sf21 cells is used. Test compound and/or vehicle is preincubated with 200 ng/ml enzyme‡ in modified HEPES buffer pH 7.4 for 15 minutes at 37°C. The reaction is initiated by addition of 0.2 mg/ml poly(Glu:Tyr), 10 μM ATP and 0.05 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:
10
Turnaround Time
Standard:
15 Business Days
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:
Taiwan - Taipei
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