Activity-based ERBB2 (R896C) kinase assay for compound screening and profiling via radiometric HotSpotTM kinase assay.
Target Overview
CAT#
ERBB2 (R896C)
Enzyme
Human ERBB2 (R896C)
HGNC
ERBB2 (R896C)
Synonym
HER2, MLN19, NEU, NGL
Scientific Information
P04626 (http://www.uniprot.org/uniprot/P04626)
Assay Properties
Substrates
Peptide substrate, poly[Glu:Tyr] (4:1), 0.2 mg/ml
ATP, 10 µM
ATP, 10 µM
Reaction
Substrate + [γ-33P]-ATP = 33P-Substrate + ADP
Readout
Enzymatic activity
Reference Compound IC50s
| Compounds | IC50 (nM) |
|---|---|
| Staurosporine | 31.7 |
| Afatinib | 1.4 |
| Gefitinib | 11.9 |
| Lapatinib | 18.1 |
| Dacomitinib | 17.8 |
Screening Location
Malvern, PA, USA
Reference compound inhibition of ERBB2 (R896C)
PDF