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Chemical Structure| 896720-20-0 Chemical Structure| 896720-20-0

Structure of VX-11e
CAS No.: 896720-20-0

Chemical Structure| 896720-20-0

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

Synonyms: TCS ERK 11e; Vertex-11e; ERK-11e

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Product Details of VX-11e

CAS No. :896720-20-0
Formula : C24H20Cl2FN5O2
M.W : 500.35
SMILES Code : FC1=CC(Cl)=C(NC2=NC(C3=CNC(C(N[C@H](CO)C4=CC=CC(Cl)=C4)=O)=C3)=C(C)C=N2)C=C1
Synonyms :
TCS ERK 11e; Vertex-11e; ERK-11e
MDL No. :MFCD18433366
InChI Key :WUTVMXLIGHTZJC-OAQYLSRUSA-N
Pubchem ID :11634725

Safety of VX-11e

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of VX-11e

MAPK

Isoform Comparison

Biological Activity

Target
  • ERK2

    ERK2, Ki:<2 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
SiHa cells 10 μM 48 hours To validate the effect of VX-11e on CKAP2 overexpression-induced cell migration and invasion, results showed that VX-11e significantly inhibited CKAP2 overexpression-induced cell migration and invasion. PMC5437009
HCT-116 cells 39 nM 96 hours VX-11e inhibits ERK in HCT-116 cells at a slightly higher concentration than ulixertinib (39 nM vs 32 nM) but exerts toxicity at a considerably lower concentration (12 nM vs 36 nM). PMC9358475
SH-SY5Y cells 50 nM 24 hours VX-11e reduced unphosphorylated ERK1/2 levels in SH-SY5Y cells but not in HCT-116 cells. PMC9358475
U937 cells 5.7 μM 96 hours VX-11e has an IC50 value of 5.7 μM in U937 cells, significantly higher than in other cell lines, indicating lower sensitivity in U937 cells. PMC9358475
MOLM-14 cells 0.625 to 40 µM 24 hours VX-11e significantly inhibited the proliferation of MOLM-14 cells and reduced ERK activation. PMC6823322
K562 cells 0.625 to 40 µM 24 hours VX-11e significantly inhibited the proliferation of K562 cells and reduced ERK activation. PMC6823322
REH cells 0.625 to 40 µM 24 hours VX-11e significantly inhibited the proliferation of REH cells and reduced ERK activation. PMC6823322
MOLT-4 cells 0.625 to 40 µM 24 hours VX-11e significantly inhibited the proliferation of MOLT-4 cells and reduced ERK activation. PMC6823322

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
NSG mice human melanoma RPDX tumors Oral gavage 50 mg/kg BID,14 days Demonstrated effective outcomes in vivo when combined with BRAF and MEK inhibitors. PMC4818716

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.00mL

0.40mL

0.20mL

9.99mL

2.00mL

1.00mL

19.99mL

4.00mL

2.00mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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