Uses
CH7057288 is a potent and selective TRK inhibitor. CH7057288 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Biological Activity
CH7057288 is a potent and selective TRK inhibitor with IC50 values of 1.1 nM, 7.8 nM and 5.1 nM for TRKA, TRKB and TRKC, respectively.
in vitro
In cell-free kinase assays, CH7057288 has selective inhibitory activity against TRKA, TRKB and TRKC, and inhibits the proliferation of cells containing TRK fusions. It inhibits MAPK and E2F signaling pathways.
target
| Target | Value |
TrkA
(Cell-free assay) | 1.1 nM |
TrkC
(Cell-free assay) | 5.1 nM |
< td style="border-bottom: 1px dotted #ccc;padding: 5px;"> TrkB
(Cell-free assay) 7.8 nM |
References
[1] Hiroshi Tanaka, et al. Abstract 4179: Potent and selective TRK inhibitor CH7057288. AACR Annual Meeting 2017; April 1-5, 2017.
