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VX-11e

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Purity:99.67%

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COA HPLC HNMR

VX-11e

Catalog No. T3166Cas No. 896720-20-0

VX-11e (TCS ERK 11e) is a potent, selective, and orally bioavailable ERK(Extracellular Signal-Regulated Kinase) inhibitor; antitumor agent.

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Pack Size	Price	Availability
2 mg	$50	In Stock
5 mg	$90	In Stock
10 mg	$124	In Stock
25 mg	$238	In Stock
50 mg	$378	In Stock
100 mg	$585	In Stock
1 mL x 10 mM (in DMSO)	$97	In Stock

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Product Introduction

Bioactivity

Description	VX-11e (TCS ERK 11e) is a potent, selective, and orally bioavailable ERK(Extracellular Signal-Regulated Kinase) inhibitor; antitumor agent.
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]
Kinase Assay	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	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)
Alias	Vertex-11e, VTX-11e, TCS ERK 11e

Chemical Properties

Molecular Weight	500.35
Formula	C24H20Cl2FN5O2
Cas No.	896720-20-0

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 50 mg/mL (100 mM)

Ethanol: 12.5 mg/mL (25 mM)

Solution Preparation Table

Ethanol/DMSO

	1mg	5mg	10mg	50mg
1 mM	1.9986 mL	9.9930 mL	19.9860 mL	99.9300 mL
5 mM	0.3997 mL	1.9986 mL	3.9972 mL	19.9860 mL
10 mM	0.1999 mL	0.9993 mL	1.9986 mL	9.9930 mL
20 mM	0.0999 mL	0.4997 mL	0.9993 mL	4.9965 mL

DMSO

	1mg	5mg	10mg	50mg
50 mM	0.0400 mL	0.1999 mL	0.3997 mL	1.9986 mL
100 mM	0.0200 mL	0.0999 mL	0.1999 mL	0.9993 mL

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