Molecular Formula | C24H20Cl2FN5O2 |
Molar Mass | 500.35 |
Density | 1.447±0.06 g/cm3(Predicted) |
pKa | 13.65±0.50(Predicted) |
Storage Condition | Keep in dark place,Inert atmosphere,Store in freezer, under -20°C |
In vitro study | In HT29 cells, VX-11e effectively inhibited cell proliferation with an IC50 of 48 nM. |
In vivo study | In both rats and mice, VX-11e showed good oral bioavailability. In NSG mice bearing human melanoma RPDX tumors, vx-11e (50 mg/kg, p.o.) resulted in strong inhibition of pRSK and inhibition of tumor growth. When used in combination with BKM120, VX-11e resulted in a significant increase in tumor growth inhibition. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 1.999 ml | 9.993 ml | 19.986 ml |
5 mM | 0.4 ml | 1.999 ml | 3.997 ml |
10 mM | 0.2 ml | 0.999 ml | 1.999 ml |
5 mM | 0.04 ml | 0.2 ml | 0.4 ml |
biological activity | VX-11e (VTX-11e, Vertex-11e) is an effective, selective, and oral bioavailable ERK2 inhibitor, Ki <2 nM, which is 200 times more selective than kinases acting on other tests. |
target | TargetValue ERK2 (Cell-free say) <2 nM(Ki) |
Target | Value |
ERK2 (Cell-free assay) | <2 nM(Ki) |
in vitro study | in HT29 cells, VX-11e effectively inhibit cell proliferation with IC50 of 48 nM. |
in vivo studies | in rats and mice, VX-11e showed good oral bioavailability. In NSG mice loaded with human melanoma RPDX tumors, VX-11e (50 mg/kg, p.o.) resulted in strong inhibition of pRSK and inhibition of tumor growth. When combined with BKM120, VX-11e leads to a significant increase in tumor growth inhibition. |