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:
676-end; G778D recombinant
Assay Information
Assay Type:
Biochemical
Assay Sub Type:
Enzymatic
Functional Mode:
Antagonist
Detection Method:
Radiometric
Measured Response:
Scintillation
Testing Information
Procedure Summary:
ErbB2 (h) is incubated with 8 mM MOPS pH 7.0, 0.2 mM EDTA, 0.1 mg/mL poly (Glu,Tyr), 5 mM MnCl2, 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 ethanol prior to drying and scintillation counting.
Substrate:
0.1 mg/mL poly (Glu,Tyr)
Tracer:
33P
ATP Concentration:
[ATP]= 10µM (Km= 6µM )
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:
Inhibition of this enzyme may be therapeutically useful in the treatment of breast and ovarian tumors.
Additional Information
Brand:
LeadHunter
Testing Location:
KP - France - Celle L'Evescault
RELATED SOLUTIONS
HER2 (ERBB2) Human RTK Kinase Enzymatic Radiometric [10 uM ATP] KinaseProfiler LeadHunter Assay - FR
Item: 14-939KP10
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