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    Pexmetinib (ARRY-614)
    Pexmetinib (ARRY-614)

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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 #: V0484
    CAS #: 945614-12-0Purity ≥98%

    Description: Pexmetinib (formerly ARRY614; ARRY-614) is a novel, potent, orally bioavailable, and dual inhibitor of p38 mitogen-activated protein kinase and Tie2 kinases with potential anti-inflammatory, anti-cancer and antiangiogenic activity. It inhibits p38 MAPK/Tie-2 kinases with IC50s of 4 nM/18 nM in a HEK-293 cell line.  

    References: Clin Cancer Res. 2015 Mar 1;21(5):985-94.

    Related CAS: 1416216-01-7 (HCl salt)

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    Molecular Weight (MW)556.63
    FormulaC31H33FN6O3
    CAS No.945614-12-0
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 100 mg/mL (179.6 mM)
    Water: <1 mg/mL
    Ethanol: N/A
    SMILESO=C(NCC1=CC(F)=CC=C1OC2=CC3=C(N(CCO)N=C3)C=C2)NC4=CC(C(C)(C)C)=NN4C5=CC=C(C)C=C5
    SynonymsARRY 614; ARRY614; ARRY-614; 1-(3-(tert-butyl)-1-(p-tolyl)-1H-pyrazol-5-yl)-3-(5-fluoro-2-((1-(2-hydroxyethyl)-1H-indazol-5-yl)oxy)benzyl)urea


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    In Vitro

    In vitro activity: In HeLa cells, Pexmetinib inhibits phospho-HSP27 with IC50 of 2 nM. In isolated PBMCs and human whole blood cells, Pexmetinib inhibits LPS-Induced TNFα with IC50 of 4.5 nM and 313 nM, respectively.


    Kinase Assay: Pexmetinib (ARRY-614) is a potent inhibitor of cytokine synthesis, via the dual inhibition of p38 mitogen-activated protein kinase (MAPK), and Tie2/Tek receptor tyrosine kinase. The in vitro IC50 values of ARR Y-614 for both Tie2 and p38 mitogen-activated protein kinase are 1000 ng/mL and 100 ng/mL, respectively.


    Cell Assay: In primary human bone marrow stromal cells, ARRY-614 inhibited basal cytokines with an IC50 value ranging from 50-100 nM.

    In VivoIn male Swiss Webster mice, Pexmetinib (30 mg/kg, p.o.) inhibits the production of the proinflammatory cytokines TNFα and IL6 in response to lipopolysaccharide (LPS) or staphyloccus enterotoxin A. In established RPMI 8226 xenografts, ARRY-614 (25 mg/kg, p.o.) inhibits tumor growth and shows additive activity when combines with thalidomide. In ovarian carcinoma A2780 xenografts, ARRY-614 (30 mg/kg, p.o.) also shows additive tumor growth inhibition activity when combines with Taxol.
    Animal modelRPMI 8226 xenografts
    Formulation & Dosage25 mg/kg; p.o.
    References

    Clin Cancer Res. 2015 Mar 1;21(5):985-94.


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

    Pexmetinib (ARRY-614)

    Bone marrow levels of p-p38 and CC3. Clin Cancer Res. 2015 Mar 1; 21(5): 985–994.

    Pexmetinib (ARRY-614)

    ARRY-614 Plasma Concentration-Time Profiles. Clin Cancer Res. 2015 Mar 1;21(5):985-94.


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