Cat. No.: HY-14178

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VX-11e

10 Cited Publications

Customer Review

Based on 10 publication(s) in Google Scholar

VX-11e is a potent, selective, and orally bioavailable inhibitor of ERK with K_i < 2 nM.

For research use only. We do not sell to patients.

Purity: 98.94%
CAS No.: 896720-20-0
Formula: C₂₄H₂₀Cl₂FN₅O₂
Molecular Weight:500.35

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

VX-11e Chemical Structure

CAS No.: 896720-20-0

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (10)
Solvent & Solubility
- In Vitro
- In Vivo
Protocol
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

VX-11e is a potent, selective, and orally bioavailable inhibitor of ERK with K_i < 2 nM.

IC₅₀ & Target^[1]

ERK2

2 nM (Ki)

GSK3

395 (Ki)

AURA

540 (Ki)

CDK2

852 (Ki)

All ERK Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
HT-29	IC₅₀	48 nM Compound: 11e	Antiproliferative activity against human HT-29 cells Antiproliferative activity against human HT-29 cells	[PMID: 19827834]

In Vitro

VX-11e is active in the HT29 cell proliferation assay (IC₅₀=48 nM)^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

VX-11e is orally bioavailable in both rat and mice^[1]. VX-11e (50 mg/kg, p.o.) results in robust inhibition of pRSK, and inhibits tumor growth in NSG mice bearing human melanoma RPDX tumors. VX-11e with BKM120 significantly improves tumor growth inhibition^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chemical Information

CAS No. 896720-20-0
Appearance Solid
Molecular Weight 500.35
Formula C₂₄H₂₀Cl₂FN₅O₂
Color White to off-white
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
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (10)

All WBCell Proliferation/Viability Assay

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Journal Impact Factor

Sci Transl Med

PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]

2018 Jul 18;10(450):eaaq1093. PMID: 30021885
Cell Rep Med

Enhanced conversion of T cells into CAR T cells by modulation of the MAPK/ERK pathway. [Abstract]

2025 Feb 6:101970. PMID: 39938523
Cell Death Dis

UBR5 targets tumor suppressor CDC73 proteolytically to promote aggressive breast cancer. [Abstract]

2022 May 12;13(5):451. PMID: 35551175
J Invest Dermatol

Inhibition of the Extracellular Signal-Regulated Kinase/Ribosomal S6 Kinase Cascade Limits Chlamydia trachomatis Infection. [Abstract]

2021 Apr;141(4):852-862.e6. PMID: 32918951
Sci Rep

Super-enhancer-driven SLCO4A1-AS1 is a new biomarker and a promising therapeutic target in glioblastoma. [Abstract]

2025 Jan 6;15(1):954. PMID: 39762261
BMC Cancer

PPP4C: a potential molecular marker and therapeutic target in thyroid cancer and triple-negative breast cancer. [Abstract]

2026 May 4;26(1):768. PMID: 42082953
Stem Cells Dev

Zinc Promotes Patient-Derived Induced Pluripotent Stem Cell Neural Differentiation via ERK-STAT Signaling. [Abstract]

2020 Jul 1;29(13):863-875. PMID: 32323639
ACS Comb Sci

Benzimidazolyl-pyrazolo[3,4- b]pyridinones, Selective Inhibitors of MOLT-4 Leukemia Cell Growth and Sea Urchin Embryo Spiculogenesis: Target Quest. [Abstract]

2019 Dec 9;21(12):805-816. PMID: 31689077
Oncotarget

MAPK1E322K mutation increases head and neck squamous cell carcinoma sensitivity to erlotinib through enhanced secretion of amphiregulin. [Abstract]

2016 Apr 26;7(17):23300-11. PMID: 27004400

VX-11e purchased from MedChemExpress. Usage Cited in: Oncotarget. 2016 Apr 26;7(17):23300-11. [Abstract]

A. HNSCC cells are treated with DMSO vehicle or VX-11e (0.5 μM) for 24 h and cell protein extracts analyzed. VX-11e inhibits phosphorylation of RSK1 in Cal33 and HSC-6. B. VX-11e inhibits phosphorylation of RSK1 in FaDu engineered cells.
J Prac Med

2016, 32 (11): 1734-1737.

VX-11e purchased from MedChemExpress. Usage Cited in: J Prac Med. 2016, 32 (11): 1734-1737.

Signaling pathways analysis of effects of BSP on RAW264.7 cells proliferation.

Solvent & Solubility

In Vitro:

DMSO : ≥ 100 mg/mL (199.86 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" means soluble, but saturation unknown.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 3.25 mg/mL (6.50 mM); Clear solution

This protocol yields a clear solution of ≥ 3.25 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (32.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 3.25 mg/mL (6.50 mM); Clear solution

This protocol yields a clear solution of ≥ 3.25 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (32.5 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Protocol

Kinase Assay^[1]

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 mol/L 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.

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Assay^[1]

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.

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration^[2]

Human melanoma RPDX tumors are expanded in vivo using NSG mice prior to the therapy experiments. Pooled tumor chunks banked from early mouse passages are implanted into 50 NSG mice (1:10 expansion). These tumors are harvested when reaching the maximum volume allowed on the protocol (1,000 mm³), digested, and banked as live cells. The larger part of this stock is retained as a master bank, and the other part is implanted at a 1:5 ratio into NSG mice to use in the therapy experiments. The expansion phase is under continuous drug pressure with PLX4720 200 ppm chemical additive diet at approximately clinical plasma levels. The plasma levels of PLX4720 (103.7 μg/mL ±3.2 after 7 days) are similar to steady-state levels in patients treated with vemurafenib 960 mg twice a day (130.6 μg/mL±71.78). When tumors have reached 200 mm³ per caliper measurement, animals are randomized into treatment groups followed by a 3-day ishout phase. Tumor size is assessed twice weekly per caliper measurement. Mice are sacrificed after two weeks of treatment or when necessary for animal welfare. Dosing is prolonged when tumor control is achieved as indicated. Tumor tissue is conserved in formalin (for FFPE) and snap-frozen in liquid N2 for protein extraction. Treatment groups are sacrificed 4 hours after last dose.

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (281 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Aronov, Alex M., et al. Structure-Guided Design of Potent and Selective Pyrimidylpyrrole Inhibitors of Extracellular Signal-Regulated Kinase (ERK) Using Conformational Control. Journal of Medicinal Chemistry (2009), 52(20), 6362-6368.

[2]. Krepler C, et al. Personalized Preclinical Trials in BRAF Inhibitor-Resistant Patient-Derived Xenograft Models Identify Second-Line Combination Therapies. Clin Cancer Res. 2016 Apr 1;22(7):1592-602. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.9986 mL	9.9930 mL	19.9860 mL	49.9650 mL
	5 mM	0.3997 mL	1.9986 mL	3.9972 mL	9.9930 mL
	10 mM	0.1999 mL	0.9993 mL	1.9986 mL	4.9965 mL
	15 mM	0.1332 mL	0.6662 mL	1.3324 mL	3.3310 mL
	20 mM	0.0999 mL	0.4997 mL	0.9993 mL	2.4983 mL
	25 mM	0.0799 mL	0.3997 mL	0.7994 mL	1.9986 mL
	30 mM	0.0666 mL	0.3331 mL	0.6662 mL	1.6655 mL
	40 mM	0.0500 mL	0.2498 mL	0.4997 mL	1.2491 mL
	50 mM	0.0400 mL	0.1999 mL	0.3997 mL	0.9993 mL
	60 mM	0.0333 mL	0.1666 mL	0.3331 mL	0.8328 mL
	80 mM	0.0250 mL	0.1249 mL	0.2498 mL	0.6246 mL
	100 mM	0.0200 mL	0.0999 mL	0.1999 mL	0.4997 mL

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VX-11e

Immunology/Inflammation Compound Library

Kinase Inhibitor Library

MAPK Compound Library

Stem Cell Signaling Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Reprogramming Compound Library

Oxygen Sensing Compound Library

Orally Active Compound Library

Glutamine Metabolism Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Obesity Compound Library

Angiogenesis-Related Compound Library

Anti-Liver Cancer Compound Library

Anti-Colorectal Cancer Compound Library

Anti-Prostate Cancer Compound Library

Anti-Pulmonary Fibrosis Compound Library

Cancer Stem Cells Compound Library

Pain-Related Compound Library

Highly Selective Inhibitors Library

Serine/Threonine Kinase Inhibitor Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Protein Kinase Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Lactylation Compound Library

Publications Citing Use of MedChemExpress (MCE) VX-11e

All ERK Isoforms

Biological Activity

Chemical Information

Publications (10)

Solvent & Solubility

Protocol

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

VX-11e Related Classifications

HY-14178 Related Classifications