EGFR Human RTK Kinase Enzymatic Radiometric LeadHunter Assay [10 μM ATP] - TW
OVERVIEW
DOCUMENTS/REFERENCES
Biological Information
Background Information:
Binding of EGF or TGFa (transforming growth factor a) to the EGF receptor results in activation of intrinsic tryrosine kinase activity. Several cytosolic proteins are phosphorylated by the EGF receptor leading to activation of signalling pathways that induce mitogenesis and, in some instances, associated cell transformation
Family:
Kinase
Sub Family:
RTK
Class:
Protein Tyrosine
Protein Name:
EGFR
Uniprot Number:
P00533
Protein Aliases:
erythroblastic leukemia viral (v-erb-b) oncogene homolog (avian)|erb-b2 receptor tyrosine kinase 1
Gene Name:
EGFR
Gene ID:
1956
Gene Aliases:
ERBB1
Accession Number:
NM_005228
Organism:
Human
Construct Details:
Fragment (668-1210), 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 EGFR expressed in insect cells is used. Test compound and/or vehicle is preincubated with 0.134 μg/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 0.25 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:
Tyrphostine AG 1478
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:
2
Turnaround Time
Standard:
15 Business Days
Reference Compound Data
Clinical Relevance
Therapeutic Area:
Oncology/Immuno-Oncology
Adverse / Beneficial Action:
Inhibitors of EGF receptor tyrosine kinase activity may be useful for chemotherapeutic intervention in cases of malignant cellular proliferation.
Additional Information
Brand:
LeadHunter
Testing Location:
Taiwan - Taipei
RELATED SOLUTIONS
DrugMatrixScreen LeadHunter Panel - TW
Item: PP89
EGFR Human RTK Kinase Binding Radiometric LeadHunter Assay [10 uM ] - TW
Item: 225510
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