Activity-based EGFR (L858R/T790M) kinase assay for compound screening and profiling via radiometric HotSpotTM kinase assay.
Target Overview
CAT#
EGFR (L858R, T790M)
Enzyme
Human EGFR (L858R, T790M)
HGNC
EGFR (T790M/L858R)
Synonym
ERBB, mENA, ERBB1
Substrates
Peptide substrate, poly[Glu:Tyr] (4:1), 0.2 mg/ml
ATP 10 µM
ATP 10 µM
Assay Properties
Reaction
Substrate + [γ-33P]-ATP = 33P-Substrate + ADP
Readout
Enzymatic activity
Reference Compound IC50s
Compounds | IC50 (nM) |
---|---|
Staurosporine | 1.6 |
PP2 | 3,800 |
AG1478 | 4,500 |
Scientific Information
P00533 (http://www.uniprot.org/uniprot/P00533)
Screening Location
Malvern, USA
Reference compound IC50 for EGFR (L858R, T790M)
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