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VX-11e

Catalog No. T3166 CAS 896720-20-0

Synonyms: Vertex-11e, VTX-11e, TCS ERK 11e

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

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

VX-11e, CAS 896720-20-0

Pack Size	Availability	Price/USD
2 mg	In stock	$ 50.00
5 mg	In stock	$ 90.00
10 mg	In stock	$ 124.00
25 mg	In stock	$ 238.00
50 mg	In stock	$ 378.00
100 mg	In stock	$ 585.00
1 mL * 10 mM (in DMSO)	In stock	$ 97.00

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Purity: 99.67%

Purity: 99.6%

Purity: 98.92%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	VX-11e (TCS ERK 11e) is a potent, selective, and orally bioavailable ERK(Extracellular Signal-Regulated Kinase) inhibitor; antitumor agent.
Targets&IC50	ERK2:<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]
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)

Synonyms	Vertex-11e, VTX-11e, TCS ERK 11e
Molecular Weight	500.35
Formula	C24H20Cl2FN5O2
CAS No.	896720-20-0

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)

References and Literature

1. Aronov AM, et al. J Med Chem. 2009, 52(20), 6362-6368. 2. Krepler C, et al. Clin Cancer Res. 2015. pii: clincanres.1762. 2015

Related compound libraries

This product is contained In the following compound libraries：

Tyrosine Kinase Inhibitor Library Inhibitor Library Highly Selective Inhibitor Library Neural Regeneration Compound Library Glutamine Metabolism Compound Library Bioactive Compound Library Epigenetics Compound Library Anti-Pancreatic Cancer Compound Library Anti-Breast Cancer Compound Library Antioxidant Compound Library

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

VX-11e 896720-20-0 Angiogenesis Cell Cycle/Checkpoint Chromatin/Epigenetic MAPK PI3K/Akt/mTOR signaling Stem Cells Tyrosine Kinase/Adaptors GSK-3 ERK Aurora Kinase CDK FLT Extracellular signal regulated kinases Inhibitor inhibit Vertex-11e VTX-11e TCS ERK 11e VX 11e VX11e inhibitor

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