CEP-40783 is a potent, selective and orally potent inhibitor of axl and c-Met with IC50 values of 7nM and 12nM, respectively.
Biological Activity
RXDX-106 (CEP-40783) is an orally available, potent, and selective inhibitor of TAM (TYRO3, AXL, MER)/Met (c-Met), with low levels in peptide phosphorylation assays. Nanomolar biochemical activity; slow dissociation rate (T1/2 >120 min) in in vitro kinase binding assays.
in vitro
CEP-40783 inhibited TAM and c-MET phosphorylation, accompanied by a decrease in downstream MAPK and PI3K signaling and cellular activity. In TAM-expressing cells, sub-nanomolar concentrations of RXDX-106 completely inhibited cell proliferation and cell viability.
in vivo
CEP-40783 inhibits tumors with activating TAM gene fusions and affects the TAM-expressing tumor microenvironment, resulting in an overall anticancer environment.