PDGFRalpha Human RTK Kinase Enzymatic Radiometric LeadHunter Assay [10 μM ATP] - TW
OVERVIEW
DOCUMENTS/REFERENCES
Biological Information
Background Information:
Receptors that are tyrosine protein kinases include those receptors for platelet-derived growth factor (PDGF), insulin, epidermal growth factor (EGF) and certain lymphokines. Receptor tyrosine kinases are cell surface transmembrane proteins responsible for intracellular signal transduction. They are expressed in several cell types and, after activation by growth factor binding, trigger a series of intracellular pathways leading to a wide variety of responses; e.g. differentiation, proliferation, migration and invasion, angiogenesis, survival. Inhibition of PDGFA, Alpha platelet-derived growth factor receptor, PDGF-R-alpha, CD140a antigen) receptor kinase may be useful in the treatment of several tumors.
Family:
Kinase
Sub Family:
RTK
Class:
Protein Tyrosine
Protein Name:
PDGFRalpha
Uniprot Number:
P16234
Protein Aliases:
PDGFR-alpha|Alpha platelet-derived growth factor receptor|Alpha-type platelet-derived growth factor receptor|CD140 antigen-like family member A|CD140a antigen|Platelet-derived growth factor alpha receptor|Platelet-derived growth factor receptor 2|PDGFR-2|CD antigen CD140a
Gene Name:
PDGFRA
Gene ID:
5156
Gene Aliases:
CD140a|PDGFR2|GAS9|RHEPDGFRA
Accession Number:
NM_006206
Organism:
Human
Construct Details:
Fragment (550-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 PDGFRA expressed in insect Sf21 cells is used. Test compound and/or vehicle is preincubated with 0.12 U/ml enzyme‡ for 15 minutes at 37°C in modified HEPES buffer pH 7.4. The reaction is initiated by addition of 0.2 mg/ml poly(Glu:Tyr), 10 µM ATP containing 0.25 µCi [γ32P]ATP for 30 minutes and terminated by further addition of 3% H3PO4. An aliquot is counted to determine the radioactivity of [32P]Poly(Glu:Tyr). 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
Additional Information
Brand:
LeadHunter
Testing Location:
Taiwan - Taipei
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