All AbMole products are for research use only, cannot be used for human consumption.
In vitro: In HT29 cells, VX-11e potently inhibits cell proliferation with IC50 of 48 nM.
In vivo: In both rats and mice, VX-11e shows good oral bioavailability. In NSG mice bearing human melanoma RPDX tumors, VX-11e (50 mg/kg, p.o.) results in robust inhibition of pRSK, and inhibits tumor growth. When used in combination with BKM120, VX-11e results in significantly improved tumor growth inhibition.
| Cell Experiment | |
|---|---|
| Cell lines | HT29 cells |
| Preparation method | Cell proliferation is measured by 3H-thymidine incorporation. The cells are plated at a concentration of 10,000 cells/well in a 96-well plate using growth media, RPMI 1640 containing 10% FBS. Serially diluted compounds are added. The cells and compounds are incubated for 48 hours at 37°C incubator. After 48 hours, 0.4 μCi of 3H-thymidine is added to each wells for 8 hours and returned to the 37°C incubator. The cells are harvested using a Tomtec 96-well cell harvester and the CPM is determined using the Wallac 1205 BETAPLATE liquid scintillation counter. The IC50 is the 50% inhibition of contr |
| Concentrations | ~10 μM |
| Incubation time | 48 h |
| Animal Experiment | |
|---|---|
| Animal models | NSG mice bearing human melanoma RPDX tumors |
| Formulation | 5% ethanol, 20% propylene glycol, 7.4% Tween80 |
| Dosages | 50 mg/kg BID |
| Administration | p.o. |
| Molecular Weight | 500.35 |
| Formula | C24H20Cl2FN5O2 |
| CAS Number | 896720-20-0 |
| Solubility (25°C) | DMSO ≥ 60 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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