FGFR2 Kinase Mutant Profiler Service

Activity-based FGFR2 mutant kinase panel for compound profiling via radiometric HotSpotTM kinase assay.
Target Overview
CAT#

FGFR2

Enzyme

Human FGFR2

HGNC

FGFR2

Synonym

Fibroblast growth factor receptor 2 [Precursor], Keratinocyte growth factor receptor 2

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 3.3 1,600 4,800 n.a. n.a. 6,000
C491A 4.1 1,100 4,400 n.a. >100,000 6,800
C491F 1.5 125 800 n.a. >100,000 1,800
C491S 3.9 520 3,400 n.a. >100,000 3,900
K526E 0.5 17 52 >50,000 n.a. 260
N549H 2.0 78.1 390 36,800 n.a. 1,200
V564F 1.6 5,500 5,000 61,000 n.a. 56
E565G 3.9 17 6.5 >50,000 n.a. 190
R612T 0.5 92 174 >100,000 n.a. 700
K641R 3.1 13 15 >50,000 n.a. 210
K659N 0.4 23 39 >50,000 n.a. 320
Screening Location

Malvern, USA