ERBB2 Kinase Mutant Profiler Service

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

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
Screening Location

Malvern, USA