Home MAPK ERK inhibitor VX-11e For research use only.

VX-11e

Synonyms: VTX-11e, Vertex-11e

VX-11e (VTX-11e, Vertex-11e) is a potent, selective, and orally bioavailable ERK inhibitor with IC50 of 17 nM (ERK1) and 15 nM (ERK2), over 200-fold selective over other kinases tested.

VX-11e Chemical Structure

VX-11e Chemical Structure

CAS No. 896720-20-0

Purity & Quality Control

Batch: S770901 DMSO]100 mg/mL]false]Ethanol]16 mg/mL]false]Water]Insoluble]false Purity: 99.22%
99.22

VX-11e Related Products

Signaling Pathway

ERK Signaling Pathways

ERK Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HT-29 cells Proliferation assay Antiproliferative activity against human HT-29 cells, IC50=0.048 μM 19827834
Click to View More Cell Line Experimental Data

Biological Activity

Description VX-11e (VTX-11e, Vertex-11e) is a potent, selective, and orally bioavailable ERK inhibitor with IC50 of 17 nM (ERK1) and 15 nM (ERK2), over 200-fold selective over other kinases tested.
Targets
ERK2 [1]
(Cell-free assay)
<2 nM(Ki)
In vitro
In vitro In HT29 cells, VX-11e potently inhibits cell proliferation with IC50 of 48 nM. [1]
Kinase Assay ERK Inhibition Assay
Compounds are assayed for the inhibition of ERK2 by a spectophotometric coupled-enzyme assay. In this assay, a fixed concentration of activated ERK2 (10 nM) is incubated with various concentrations of the compounds in DMSO (2.5%) for 10 min. at 30 °C in 0.1 M HEPES buffer, pH = 7.5, containing 10 mM MgCl2, 2.5 mM phosphoenolpyruvate, 200 μM NADH, 150 μg/mL pyruvate kinase, 50 μg/mL lactate dehydrogenase and 200 μM erktide peptide. The reaction is initiated by the addition of 65 μM ATP. The rate of decrease of absorbance at 340 nM is monitored. The IC50 is evaluated from the data as a function of inhibitor concentr
Cell Research Cell lines HT29 cells
Concentrations ~10 μM
Incubation Time 48 h
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
In Vivo
In vivo In both rats and mice, VX-11e shows good oral bioavailability. [1] 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. [2]
Animal Research Animal Models NSG mice bearing human melanoma RPDX tumors
Dosages 50 mg/kg BID
Administration p.o.

Chemical Information & Solubility

Molecular Weight 500.35 Formula

C24H20Cl2FN5O2
CAS No. 896720-20-0 SDF Download VX-11e SDF
Smiles CC1=CN=C(N=C1C2=CNC(=C2)C(=O)NC(CO)C3=CC(=CC=C3)Cl)NC4=C(C=C(C=C4)F)Cl
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 100 mg/mL ( (199.86 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 16 mg/mL

Water : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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