VX-11e

Catalog No.S7709 Batch:S770901

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Technical Data

Formula

C24H20Cl2FN5O2
Molecular Weight 500.35 CAS No. 896720-20-0
Solubility (25°C)* In vitro DMSO 100 mg/mL (199.86 mM)
Ethanol 16 mg/mL (31.97 mM)
Water Insoluble
In vivo (Add solvents to the product individually and in order)
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
5.0mg/ml Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to make it clear; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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 HT29 cells, VX-11e potently inhibits cell proliferation with IC50 of 48 nM. [1]
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]

Protocol (from reference)

Kinase Assay:[1]
  • 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 Assay:[1]
  • 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
Animal Study:[2]
  • Animal Models

    NSG mice bearing human melanoma RPDX tumors

  • Dosages

    50 mg/kg BID

  • Administration

    p.o.

Selleck's VX-11e has been cited by 26 publications

MAPK1 Mediates MAM Disruption and Mitochondrial Dysfunction in Diabetic Kidney Disease via the PACS-2-Dependent Mechanism [ Int J Biol Sci, 2024, 20(2):569-584] PubMed: 38169625
Integrated drug response prediction models pinpoint repurposed drugs with effectiveness against rhabdomyosarcoma [ PLoS One, 2024, 19(1):e0295629] PubMed: 38277404
Kinase-Modulated Bioluminescent Indicators Enable Noninvasive Imaging of Drug Activity in the Brain [ ACS Cent Sci, 2023, 9(4):719-732] PubMed: 37122464
ERK2-topoisomerase II regulatory axis is important for gene activation in immediate early genes [ Nat Commun, 2023, 14(1):8341] PubMed: 38097570
ERK1/2 inhibitors act as monovalent degraders inducing ubiquitylation and proteasome-dependent turnover of ERK2, but not ERK1 [ Biochem J, 2023, 480(9):587-605] PubMed: 37018014
miR-125b-5p-MAPK1-C/EBPα feedback loop regulates all-trans retinoic acid resistance in acute promyelocytic leukemia [ Gene, 2023, 889:147806] PubMed: 37717613
ERK Hyperactivation Serves as a Unified Mechanism of Escape in Intrinsic and Acquired CDK4/6 Inhibitor Resistance in Acral Lentiginous Melanoma [ Res Sq, 2023, rs.3.rs-2817876] PubMed: 37131684
Conformation Selection by ATP-competitive Inhibitors and Allosteric Communication in ERK2 [ bioRxiv, 2023, 2023.09.12.557258] PubMed: 37745518
Identification of cell type-specific correlations between ERK activity and cell viability upon treatment with ERK1/2 inhibitors [ J Biol Chem, 2022, 298(8):102226] PubMed: 35787369
Establishment and characterization of immortalized sweat gland myoepithelial cells [ Sci Rep, 2022, 12(1):7] PubMed: 34997030

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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