1. MAPK/ERK Pathway
    Stem Cell/Wnt
  2. ERK

VX-11e 

Cat. No.: HY-14178 Purity: 98.68%
Data Sheet SDS Handling Instructions

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 (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO $109 In-stock
5 mg $99 In-stock
10 mg $125 In-stock
50 mg $400 In-stock
100 mg $700 In-stock
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

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

    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.
    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

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

    In Vitro

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

    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].

    References
    Preparing Stock Solutions
    Concentration Volume 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
    10 mM 0.1999 mL 0.9993 mL 1.9986 mL
    Please refer to the solubility information to select the appropriate solvent.
    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]

    VX-11e is suspended in 5% ethanol, 20% propylene glycol, 7.4% Tween 80. 

    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
    Molecular Weight

    500.35

    Formula

    C₂₄H₂₀Cl₂FN₅O₂

    CAS No.

    896720-20-0

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Shipping

    Room temperature in continental US; may vary elsewhere

    Solvent & Solubility

    10 mM in DMSO

    * "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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    Inquiry Information

    Product Name:
    VX-11e
    Cat. No.:
    HY-14178
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