FLT3 Kinase Mutant Profiler Service

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

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
F594_R595insR 0.4 3,400 130 64 n.a. 35
F594_R595insREY 0.6 3,950 174 70 n.a. 35
R595_E596insEY 0.5 3,500 160 50 n.a. 24
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, USA