Home MAPK ERK inhibitor VX-11e

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VX-11e ERK inhibitor

Cat.No.S7709

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 ERK inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 500.35

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Quality Control

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

Cell Culture, Treatment & Working Concentration

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
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Solubility

In vitro
Batch:

DMSO : 100 mg/mL (199.86 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 16 mg/mL

Water : Insoluble

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Mass Concentration Volume Molecular Weight
Dilution Calculator Molecular Weight Calculator

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Chemical Information, Storage & Stability

Molecular Weight 500.35 Formula

C24H20Cl2FN5O2

 Storage (From the date of receipt)
CAS No. 896720-20-0 Download SDF Storage of Stock Solutions

Synonyms VTX-11e, Vertex-11e 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

Mechanism of Action

Targets/IC50/Ki
ERK2
(Cell-free assay)
<2 nM(Ki)
ERK1
17 nM
In vitro
In HT29 cells, VX-11e potently inhibits cell proliferation with IC50 of 48 nM.
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 concentration.
In vivo
In both rats and mice, VX-11e shows good oral bioavailability. In NSG mice bearing human melanoma RPDX tumors, this compound (50 mg/kg, p.o.) results in robust inhibition of pRSK, and inhibits tumor growth. When used in combination with BKM120, this chemical results in significantly improved tumor growth inhibition.
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