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 |
| C491S/V564L | 0.1 | >100,000 | >100,000 | n.a. | >100,000 | 780 |
| V564L | 0.3 | >100,000 | >100,000 | n.a. | >100,000 | 820 |
Screening Location
Malvern, PA, USA