VX-11e

Catalog No.S7709 Synonyms: VTX-11e, Vertex-11e

VX-11e  Chemical Structure

Molecular Weight(MW): 500.35

VX-11e is a potent, selective, and orally bioavailable ERK2 inhibitor with Ki of <2 nM, over 200-fold selective over other kinases tested.

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Biological Activity

Description VX-11e is a potent, selective, and orally bioavailable ERK2 inhibitor with Ki of <2 nM, 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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HT-29 cells MmrRVJJwdGmoZYLheIlwdiCjc4PhfS=> MlnFRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKVD2yPUBk\WyuczygTWM2OD1yLkC0PEDPxE1? M2fPc|E6QDJ5OEO0

... Click to View More Cell Line Experimental Data

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

Kinase Assay:[1]
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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 Research:[1]
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  • 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
    (Only for Reference)
Animal Research:[2]
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  • Animal Models: NSG mice bearing human melanoma RPDX tumors
  • Formulation: 5% ethanol, 20% propylene glycol, 7.4% Tween80
  • Dosages: 50 mg/kg BID
  • Administration: p.o.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL (199.86 mM)
Ethanol 16 mg/mL (31.97 mM)
Water 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.

Chemical Information

Molecular Weight 500.35
Formula

C24H20Cl2FN5O2

CAS No. 896720-20-0
Storage powder
in solvent
Synonyms VTX-11e, Vertex-11e

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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ERK Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID