[CAS NO. 896720-20-0] VX-11e
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PRODUCTS SPECIFICATIONS [896720-20-0]
Store
Catalog
SLK-S7709
Brand
Selleck
CAS
896720-20-0
DESCRIPTION [896720-20-0]
Overview
| MDL | MFCD18433366 |
|---|---|
| Molecular Weight | 500.35 |
| Molecular Formula | C24H20Cl2FN5O2 |
| SMILES | FC1=CC(Cl)=C(NC2=NC(C3=CNC(C(N[C@H](CO)C4=CC=CC(Cl)=C4)=O)=C3)=C(C)C=N2)C=C1 |
For research use only.
Storage
3 years,-20°C,powder
1 years,-80°C,in solvent
1 years,-80°C,in solvent
Shipping
Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)
Preparing Stock Solutions
| 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9986 mL | 9.9930 mL | 19.9860 mL |
| 5 mM | 0.3997 mL | 1.9986 mL | 3.9972 mL |
| 10 mM | 0.1999 mL | 0.9993 mL | 1.9986 mL |
| 50 mM | 0.0400 mL | 0.1999 mL | 0.3997 mL |
Description
VX-11e (VTX-11e, Vertex-11e) is a potent, selective, and orally bioavailable inhibitor with of <2 nM, over 200-fold selective over other kinases tested.
Targets
| ERK2 [1] (Cell-free assay) |
| <2 nM(Ki) |
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.
References
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