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Angiogenesis FLT VX-11e

VX-11e

Catalog No. T3166
Synonyms: VTX-11e, Vertex-11e, TCS ERK 11e
Purity 98.00% Datasheet

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

VX-11e, CAS 896720-20-0
Pack Size Availability Price/USD Quantity
2 mg In stock 56.00
5 mg In stock 101.00
10 mg In stock 147.00
25 mg In stock 264.00
50 mg In stock 419.00
100 mg In stock 651.00
1 mL * 10 mM (in DMSO) In stock 130.00
Bulk Size: Please Quote for Discount
Purity 98.00%
Purity 98.92%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description VX-11e is a potent, selective, and orally bioavailable ERK(Extracellular Signal-Regulated Kinase) inhibitor; antitumor agent.
Targets&IC50 Aurora A :ic50 540nM(Ki),   CDK2 :ic50 850nM(Ki),   ERK2 :ic50 <2nM(Ki),   FLT3 :ic50 1.4μM(Ki),   GSK-3 :ic50 400nM(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)
Cell lines: HT29 cells
Animal Research
Animal Model: NSG mice bearing human melanoma RPDX tumors

Description

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

Targets&IC50

Aurora A :ic50 540nM(Ki)

CDK2 :ic50 850nM(Ki)

ERK2 :ic50 <2nM(Ki)

FLT3 :ic50 1.4μM(Ki)

GSK-3 :ic50 400nM(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)

Cell lines: HT29 cells

Animal Research

Animal Model: NSG mice bearing human melanoma RPDX tumors

Synonyms VTX-11e, Vertex-11e, TCS ERK 11e
Purity 98.92%
Appearance solid
Molecular Weight 500.35
Formula C24H20Cl2FN5O2
CAS No. 896720-20-0
SMILES data to be upload

Storage

Powder: -20°C, 3years; 4°C, 2 years

In solvent: -80°C, 6 months; -20°C, 1 month

Solubility Information

DMSO: 50 mg/mL (100 mM)

Ethanol: 12.5 mg/mL (25 mM)

( < 1 mg/ml refers to the product slightly soluble or insoluble )

Citations

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:
Bioactive Compound Library Inhibitor Library Anti-cancer Compound Library Stem cell Differentiation Compound Library Epigenetics Compound Library MAPK Inhibitor Library Oxidation-Reduction Compound Library PI3K-AKT-mTOR Compound Library Tyrosine kinase Inhibitor Library Kinase Inhibitor Library Fluorochemical Library Angiogenesis related Compound Library Cell cycle related Compound Library

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MSC2530818 AC710 Tesevatinib CDK inhibitor II NVP-LCQ195 LY2857785 Ilorasertib Ilorasertib

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