Activity-based FGFR3 mutant kinase panel for compound profiling via radiometric HotSpotTM kinase assay.
Target Overview
CAT#
FGFR3
Enzyme
Human FGFR3
HGNC
FGFR3
Synonym
Fibroblast growth factor receptor 3 [Precursor], FGFR-3
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 | 25 | 9,200 | 22,000 | n.a. | n.a. | 9,000 |
| V555M | 1.8 | >100,000 | >100,000 | 77,000 | n.a. | 5,400 |
| G697C | 3.4 | 3,000 | 6,500 | 18,000 | n.a. | 6,000 |
| K650E | 5.1 | 6,100 | 3,700 | n.a. | n.a. | 11,200 |
| K650M | 20 | 2,000 | 2,200 | >50,000 | n.a. | 11,000 |
| K650Q | 20 | 1,300 | 1,800 | >50,000 | n.a. | 12,000 |
Screening Location
Malvern, USA
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