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    VX-11e
    VX-11e

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V0468
    CAS #: 896720-20-0Purity ≥98%

    Description: VX-11e is a novel, potent, selective, and orally bioavailable ERK2 (extracellular signal-related kinase 2) inhibitor with potential anticancer activity. It inhibits ERK2 with a Ki of<2 which='' is=''>200-fold more selective over other kinases. ERK is extracellular signal-regulated kinases, and is a key component of the Ras/Raf/MEK/ERK signal transduction pathway, which is an oncogenic pathway related to a variety of human cancers. In both rats and mice, VX-11e shows good oral bioavailability. 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.

    References: J Med Chem. 2009 Oct 22;52(20):6362-8; Clin Cancer Res. 2016 Apr 1;22(7):1592-602. 

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    Molecular Weight (MW)500.35
    FormulaC24H20Cl2FN5O2
    CAS No.896720-20-0
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 100 mg/mL (199.9 mM)
    Water: <1 mg/mL
    Ethanol: 16 mg/mL (32.0 mM)
    SMILESO=C(C1=CC(C2=NC(NC3=CC=C(F)C=C3Cl)=NC=C2C)=CN1)N[[email protected]@H](C4=CC=CC(Cl)=C4)CO
    SynonymsTCS ERK 11e;  TCS ERK-11e;  TCS ERK11e;  ERK-11e; ERK 11e; ERK11e; VTX-11e, Vertex-11e; VX-11e; VX 11e; VX11e; VTX-11e; VTX11e; VTX 11e


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    In Vitro

    In vitro activity: In HT29 cells, VX-11e potently inhibits cell proliferation with IC50 of 48 nM.


    Kinase Assay: Compounds were assayed for the inhibition of ERK2 by a spectophotometric coupled-enzyme assay. In this assay, a fixed concentration of activated ERK2 (10 nM) was incubated with various concentrations of the compounds in DMSO (2.5%) for 10 mins at 30 ℃ 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 was initiated by the addition of 65 μM ATP. The rate of decrease of absorbance at 340 nM was monitored. The IC50 was evaluated from the data as a function of inhibitor concentration.


    Cell Assay: 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.

    In Vivo In both rats and mice, VX-11e shows good oral bioavailability. 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
    Animal modelNSG mice bearing human melanoma RPDX tumors 
    Formulation & DosageFormulated in 5% ethanol, 20% propylene glycol, 7.4% Tween80; 50 mg/kg; p.o.
    References

    J Med Chem. 2009 Oct 22;52(20):6362-8; Clin Cancer Res. 2016 Apr 1;22(7):1592-602. 


    These protocols are for reference only. InvivoChem does not independently validate these methods.

    VX-11e

     


    VX-11e

    Journal of Medicinal Chemistry (2009), 52(20), 6362-6368.

     VX-11e


    dual pathway inhibition controls tumor growth.  2016 Apr 1;22(7):1592-602.


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