Activity-based FGFR4 mutant kinase panel for compound profiling via radiometric HotSpotTM kinase assay.
Target Overview
CAT#
FGFR4
Enzyme
Human FGFR4
HGNC
FGFR4
Synonym
Fibroblast growth factor receptor 4 [Precursor], FGFR-4, JTK2, TKF
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 | 110 | 2,400 | >20,000 | n.a. | n.a. | >20,000 |
| N535K | 4,800 | 22,000 | 27,000 | n.a. | >100,000 | >100,000 |
| V550E | 3,700 | >100,000 | >100,000 | n.a. | >100,000 | >100,000 |
| V550L | 70 | >100,000 | >100,000 | >100,000 | n.a. | >100,000 |
| V550M | 28 | >100,000 | >100,000 | 70,000 | n.a. | 95,000 |
Screening Location
Malvern, USA
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