Activity-based FLT3 mutant kinase panel for compound profiling via radiometric HotSpotTM kinase assay.
Target Overview
CAT#
FLT3
Enzyme
Human FLT3
HGNC
FLT3
Synonym
FL cytokine receptor [Precursor], Tyrosine-protein kinase receptor FLT3, Stem cell tyrosine kinase 1, STK-1, Flk-2
Scientific Information
P36888 (http://www.uniprot.org/uniprot/P36888)
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 | 2.2 | 2,900 | 320 | 302 | n.a. | 56.5 |
| Y591_V592insVDFREYEYD | 0.9 | 2,300 | 190 | 150 | n.a. | 18 |
| Y591-V592insVDFREYEYD/F691L | 0.3 | 51,000 | 2,200 | n.a. | >100,000 | 89 |
| Y591-V592insVDFREYEYD/D835Y | 0.7 | 1,600 | 150 | n.a. | >100,000 | 16 |
| F594_R595insR | 0.4 | 3,400 | 130 | 64 | n.a. | 35 |
| F594_R595insREY | 0.6 | 3,950 | 174 | 70 | n.a. | 35 |
| F691L/D835Y | 0.4 | >100,000 | 2,800 | n.a. | >100,000 | 220 |
| R595_E596insEY | 0.5 | 3,500 | 160 | 50 | n.a. | 24 |
| F691L | 0.6 | 37,000 | 5,800 | n.a. | >100,000 | 320 |
| D835Y | <0.1 | 9,000 | 143 | 22,800 | n.a. | 80.8 |
| ITD | <0.1 | 900 | 87 | 27 | n.a. | 4.6 |
| ITD-NPOS | 4.1 | 10,000 | 730 | 310 | n.a. | 55 |
| ITD-W51 | 1.2 | 3,600 | 250 | 94 | n.a. | 32 |
Screening Location
Malvern, PA, USA
Further Information
More information can be found on our website Kinase Assays
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