Activity-based EGFR (K716A/T790M/C797S/L858R) kinase assay for compound screening and profiling via radiometric HotSpotTM kinase assay.
Target Overview
CAT#
EGFR (K716A/T790M/C797S/L858R)
Enzyme
Human EGFR (K716A/T790M/C797S/L858R)
HGNC
EGFR (K716A/T790M/C797S/L858R)
Synonym
Epidermal growth factor receptor, Receptor tyrosine-protein kinase ErbB-1, HER1, EGF-R, ERBB, mENA, ERBB1
Substrates
Peptide substrate, poly[Glu:Tyr] (4:1), 0.2 mg/ml
ATP 10 µM
Assay Properties
Reaction
Substrate + [γ-33P]-ATP = 33P-Substrate + ADP
Readout
Enzymatic activity
Reference Compound IC50s
| Compounds | IC50 (nM) |
|---|---|
| Staurosporine | 1.2 |
| PP2 | 1,200 |
| AG1478 | 1,100 |
| EGFR/ErbB Inhibitor | >100,000 |
| D-64406 | 26,000 |
Scientific Information
P00533 (http://www.uniprot.org/uniprot/P00533)
Screening Location
Malvern, USA
Reference compound IC50 for EGFR (K716A/T790M/C797S/L858R)
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