1. MAPK/ERK Pathway Stem Cell/Wnt
  2. ERK
  3. VX-11e

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

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

VX-11e Chemical Structure

VX-11e Chemical Structure

CAS No. : 896720-20-0

Size Price Stock Quantity
Free Sample (0.1 - 0.5 mg)   Apply Now  
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 131 In-stock
Solution
10 mM * 1 mL in DMSO USD 131 In-stock
Solid
5 mg USD 119 In-stock
10 mg USD 150 In-stock
25 mg USD 300 In-stock
50 mg USD 450 In-stock
100 mg USD 720 In-stock
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Customer Review

Based on 10 publication(s) in Google Scholar

Other Forms of VX-11e:

Top Publications Citing Use of Products

    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.

    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.

    View All ERK Isoform Specific Products:

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

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

    IC50 & Target

    ERK2

    2 nM (Ki)

    GSK3

    395 (Ki)

    AURA

    540 (Ki)

    CDK2

    852 (Ki)

    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.

    Molecular Weight

    500.35

    Formula

    C24H20Cl2FN5O2

    CAS No.
    Appearance

    Solid

    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
    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.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 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
    View the Complete Stock Solution Preparation Table

    * 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

    • Dilution Calculator

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

    Mass
    =
    Concentration
    ×
    Volume
    ×
    Molecular Weight *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    In Vivo:

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

    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.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • 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

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    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).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation

    Purity: 99.17%

    References
    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.

    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.

    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.

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

    References

    Complete Stock Solution Preparation Table

    * 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.

    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 Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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