Activity-based ERBB2 mutant kinase panel for compound profiling via radiometric HotSpotTM kinase assay.
Target Overview
CAT#
ERBB2
Enzyme
Human ERBB2
HGNC
ERBB2
Synonym
Receptor tyrosine-protein kinase erbB-2 [Precursor], p185erbB2, C-erbB-2, NEU proto-oncogene, Tyrosine kinase-type cell surface receptor HER2, MLN 19
Scientific Information
P04626 (http://www.uniprot.org/uniprot/P04626)
Assay Properties
Reaction
Substrate + [γ-33P]-ATP = 33P-Substrate + ADP
Readout
Enzymatic activity
Reference Compound IC50s (nM)
| Mutant | Staurosporine | PP2 | AG1478 | PDGFR I-III | EGFR/ErbB Inhibitor | D-64406 |
|---|---|---|---|---|---|---|
| WT | 60 | 230 | 6.5 | n.a. | 0.1 | >100,000 |
| D769H | 55 | 370 | 4.7 | >100,000 | n.a. | 46,000 |
| D769Y | 23 | 470 | 19 | >100,000 | n.a. | 57,000 |
| A775_G776insYVMA | 53 | 26 | 4.6 | n.a. | 0.2 | 7,900 |
| V777-G778insCG | 140 | 25 | 3.7 | >100,000 | n.a. | 39,000 |
| V777L | 43 | 250 | 18 | >100,000 | n.a. | 54,000 |
| P780-Y781insGSP | 10 | >100,000 | 14,400 | >100,000 | n.a. | >100,000 |
| R896C | 61 | 540 | 30 | >100,000 | n.a. | >100,000 |
| P1170A | 88 | 250 | 9.3 | n.a. | 0.3 | >100,000 |
| V956R | 620 | 510 | 120 | n.a. | 0.8 | >100,000 |
Screening Location
Malvern, PA, USA
Further Information
More information can be found on our website Kinase Assays
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