ErbB2 (HER2) Human RTK Kinase Enzymatic Radiometric LeadHunter Assay [10 μM ATP] - TW
OVERVIEW
DOCUMENTS/REFERENCES
Biological Information
Background Information:
Human EGF receptor 2 (HER2, ERBB2) tyrosine kinase is an EGF receptor-related protein tyrosine kinase which is overexpressed in many mammary and ovarian carcinomas. Binding of the ligand to the receptor is believed to activate the receptor’s intrinsic protein kinase activity, initiating a signal transduction pathway which leads to increased cell proliferation. Truncated HER2, lacking the extracellular and transmembrane regions, is constitutively active. The active kinase transfers g-phosphates of ATP to the phenolic hydroxyl of specific tyrosine residues on target proteins.
Family:
Kinase
Sub Family:
RTK
Class:
Protein Tyrosine
Protein Name:
HER2
Uniprot Number:
P04626
Protein Aliases:
neuro/glioblastoma derived oncogene homolog|human epidermal growth factor receptor 2
Gene Name:
ERBB2
Gene ID:
2064
Gene Aliases:
NEU|HER-2|CD340|HER2
Accession Number:
NM_004448
Organism:
Human
Construct Details:
Fragment (676-1255), 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 ERBB2 (HER2) expressed in insect cells is used. Test compound and/or vehicle is with 1.1 μg/ml enzyme‡ in modified Tris buffer pH 7.5 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 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:
2
Turnaround Time
Standard:
15 Business Days
Reference Compound Data
Clinical Relevance
Therapeutic Area:
Oncology/Immuno-Oncology
Adverse / Beneficial Action:
Inhibition of this enzyme may be therapeutically useful in the treatment of breast and ovarian tumors.
Additional Information
Brand:
LeadHunter
Testing Location:
Taiwan - Taipei
RELATED SOLUTIONS
DrugMatrixScreen LeadHunter Panel - TW
Item: PP89
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