Molecular Formula | C31H26F2N4O6 |
Molar Mass | 588.56 |
Density | 1.394±0.06 g/cm3(Predicted) |
pKa | 10.42±0.70(Predicted) |
Storage Condition | -20℃ |
In vitro study | RXDX-106 inhibits TAM and c-MET phosphorylation, accompanied by a decrease in downstream MAPK and PI3K signaling and cellular activity. In TAM-expressing cells, subnanomolar concentrations of RXDX-106 completely inhibited cell proliferation and cell viability. |
In vivo study | RXDX-106 can inhibit tumors with activated TAM gene fusions and affect the TAM-expressing tumor microenvironment, thereby forming an overall anti-cancer environment. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 1.699 ml | 8.495 ml | 16.991 ml |
5 mM | 0.34 ml | 1.699 ml | 3.398 ml |
10 mM | 0.17 ml | 0.85 ml | 1.699 ml |
5 mM | 0.034 ml | 0.17 ml | 0.34 ml |
biological activity | RXDX-106 (CEP-40783) is an orally available, effective, selective TAM(TYRO3, AXL, MER)/Met (c-Met) inhibitor had lower nanomolar biochemical activity in the peptide Phosphorylation Assay; there was a slow dissociation rate in the in vitro Kinase binding assay (T1/2 >120 min). |
Target | Value |
Axl (Cell-free assay) | 7 nM |
c-Met (Cell-free assay) | 12 nM |
Tyro3 (Cell-free assay) | 19 nM 29 nM |
MER (Cell-free assay) | 29 nM |
Use | a potent, selective and orally effective inhibitor of axl and c-Met with IC50 values of 7nm and 12nm, respectively. |