Activity-based EGFR (T790M/C797G/L858R) kinase assay for compound screening and profiling via radiometric HotSpotTM kinase assay.
Target Overview
CAT#
EGFR (T790M/C797G/L858R)
Enzyme
Human EGFR (T790M/C797G/L858R)
HGNC
EGFR (T790M/C797G/L858R)
Synonym
Epidermal growth factor receptor, Receptor tyrosine-protein kinase ErbB-1, HER1
Scientific Information
P00533 (http://www.uniprot.org/uniprot/P00533)
Assay Properties
Substrates
Peptide substrate, poly[Glu:Tyr] (4:1), 0.2 mg/mL
ATP, 10 µM
Reaction
Substrate + [γ-33P]-ATP = 33P-Substrate + ADP
Readout
Enzymatic activity
Reference Compound IC50s
| Compounds | IC50 (nM) |
|---|---|
| Staurosporine | 0.7 |
| PP2 | 2,800 |
| AG1478 | 1,900 |
| EGFR/ErbB Inhibitor | >1,000 |
| D-64406 | 67,000 |
Screening Location
Malvern, PA, USA
Further Information
More information can be found on our website Kinase Assays
Reference compound IC50 for EGFR (T790M/C797G/L858R)
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