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
Scientific Information
P10721 (http://www.uniprot.org/uniprot/P10721)
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 | 0.9 | n.a. | 3,100 | n.a. | n.a. | 100 |
| V559A | 0.3 | 4.4 | 790 | 0.9 | n.a. | 135 |
| V559D | 0.7 | 11 | 2,000 | 3.2 | n.a. | 2,000 |
| V559D/T670I | <0.1 | 58,000 | 3,000 | 120 | n.a. | 6,200 |
| V559D/V654A | 3.0 | 2,000 | 6,100 | 160 | n.a. | 2,200 |
| V560G | 1.8 | 35 | 2,000 | 3.4 | n.a. | 111 |
| V560G/D816V | 0.4 | 6.9 | 2,000 | 15 | n.a. | 500 |
| V560G/N822K | 0.4 | 12 | 1,500 | 23 | n.a. | 1,000 |
| d557-558/Y823D | 0.6 | 5.9 | 400 | n.a. | 17,000 | 960 |
| d557-558 | 0.4 | 8.1 | 560 | 4.5 | n.a. | 70 |
| K642E | 2.9 | 280 | 24,000 | 130 | n.a. | 530 |
| V654A | 12 | 3,800 | 14,600 | 2,100 | n.a. | 144 |
| T670I | 2.3 | >100,000 | 3,800 | 796 | n.a. | 2,800 |
| D816E | <1.0 | 27 | 1,950 | 44 | n.a. | 1,100 |
| D816F | <1.0 | 36 | 3,400 | 330 | n.a. | 2,300 |
| D816H | 0.5 | 14.8 | 3,000 | 56.2 | n.a. | 1,900 |
| D816I | 0.5 | 37 | 3,800 | 76 | n.a. | 1,800 |
| D816V | 0.6 | 45.5 | 4,200 | 75.6 | n.a. | 1,800 |
| D816Y | <1.0 | 30 | 2,300 | 120 | n.a. | 1,300 |
| D820E | 1.6 | 23 | 5,700 | 34 | n.a. | 4,800 |
| D820Y | 0.3 | 9.3 | 950 | 5.4 | n.a. | 650 |
| Y823D | 1.3 | 3.6 | 710 | 3.0 | n.a. | 1,300 |
| A829P | 1.2 | 4.5 | 1,900 | 3.0 | n.a. | 1,600 |
Screening Location
Malvern, PA, USA
Further Information
More information can be found on our website Kinase Assays
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