c-KIT Kinase Mutant Profiler Service

Activity-based c-KIT mutant kinase panel for compound profiling via radiometric HotSpotTM kinase assay.
Target Overview
CAT#

c-Kit

Enzyme

Human c-Kit

HGNC

KIT

Synonym

Mast/stem cell growth factor receptor Kit, Proto-oncogene tyrosine-protein kinase c-Kit

Assay Properties
Reaction

Substrate + [γ-33P]-ATP = 33P-Substrate + ADP

Readout

Enzymatic activity

Reference Compound IC50s (nM)
Mutant Staurosporine PP2 AG1478 PDGFR I-III D-64406
WT 0.9 n.a. 3,100 n.a. 100
V559A 0.3 4.4 790 0.9 135
V559D 0.7 11 2,000 3.2 2,000
V559D/T670I <0.1 58,000 3,000 120 6,200
V559D/V654A 3.0 2,000 6,100 160 2,200
V560G 1.8 35 2,000 3.4 111
V560G/D816V 0.4 6.9 2,000 15 500
V560G/N822K 0.4 12 1,500 23 1,000
d557-558 0.4 8.1 560 4.5 70
K642E 2.9 280 24,000 130 530
V654A 12 3,800 14,600 2,100 144
T670I 2.3 >100,000 3,800 796 2,800
D816E <1.0 27 1,950 44 1,100
D816F <1.0 36 3,400 330 2,300
D816H 0.5 14.8 3,000 56.2 1,900
D816I 0.5 37 3,800 76 1,800
D816V 0.6 45.5 4,200 75.6 1,800
D816Y <1.0 30 2,300 120 1,300
D820E 1.6 23 5,700 34 4,800
D820Y 0.3 9.3 950 5.4 650
Y823D 1.3 3.6 710 3.0 1,300
A829P 1.2 4.5 1,900 3.0 1,600
Screening Location

Malvern, USA