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    BI-847325
    BI-847325

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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 #: V0350
    CAS #: 1207293-36-4Purity ≥98%

    Description: BI-847325 (BI847325) is a novel, potent, orally bioavailable, and selective dual inhibitor of MEK (mitogen-activated protein kinase kinase) and Aurora kinase with potential antitumor activity. It inhibits Aurora B, human Aurora A, Aurora C, MEK1 and MEK2 with IC50 of 3 nM, 25 nM, 15 nM, 25 nM, and 4 nM, respectively. BI 847325 shows potent in vitro antiproliferative activity and high in vivo antitumor efficacy.

    References: Mol Cancer Ther. 2015 Jun;14(6):1354-64.

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    Molecular Weight (MW)464.56
    FormulaC29H28N4O2
    CAS No.1207293-36-4
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 19 mg/mL (40.9 mM)
    Water: <1 mg/mL
    Ethanol: <1 mg/mL
    Solubility (In vivo)2-hydroxyethyl cellulose, polysorbate 80 with pH adjusted to 2.8 with 1 M HCl: 30 mg/mL
    SynonymsBI 847325; BI847325; BI-847325; (Z)-3-(3-((4-((dimethylamino)methyl)phenylamino)(phenyl)methylene)-2-oxoindolin-6-yl)-N-ethylpropiolamide


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    In Vitro

    In vitro activity: BI-847325 shows growth-inhibitory effects on BRAF-mutant and vemurafenib-resistant melanoma cells with IC50 ranging from 0.3 nM to 2 μM, and prevents colony formation in six BRAF-mutant melanoma cell lines. BI-847325 also induces apoptosis by reducing Mcl-1 expression


    Kinase Assay: BI-847325 is an ATP competitive dual inhibitor of MEK and aurora kinases (AK) with IC50 values of 15 and 4 nM for human AK-C and MEK2, respectively.


    Cell Assay: Cells (M229, M229R, A375, A375R, WM793, WM793R, 1205Lu, 1205LuR, M249, M249R, WM164, WM164R, WM39 and RPMI17951 cells) are plated at a density of 2.5 × 103 cells per 100 μL and left to grow overnight before being treated with increasing concentrations of BI-847325 for 72 hours. The metabolic activity is determined using Alamar blue reagent as per the manufacturer's protocol.

    In VivoIn mice bearing 1205Lu and 1205LuR xenografts, BI-847325 (75 mg/kg, p.o.) causes significant tumor suppression without significant alteration in the body weights
    Animal modelMice bearing 1205Lu and 1205LuR xenografts
    Formulation & DosageDissolved in  2-hydroxyethyl cellulose, polysorbate 80 with pH adjusted to 2.8 with 1 M HCl; 70 mg/kg;  Oral gavage
    References

    Mol Cancer Ther. 2015 Jun;14(6):1354-64.


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

    BI-847325

    The dual MEK and Aurora kinase inhibitor BI-847325 blocks the growth and survival of BRAF-mutant melanoma cell lines through induction of apoptosis.  2015 Jun;14(6):1354-64.


    BI-847325

    BI-847325 induces apoptosis altering the expression of pro and anti-apoptotic proteins.  2015 Jun;14(6):1354-64.

    BI-847325

    Decreased expression of Mcl-1 is required for BI-847325-mediated apoptosis.  2015 Jun;14(6):1354-64.

    BI-847325

    BI-847325-mediated apoptosis is induced following downregulation of Mcl-1.  2015 Jun;14(6):1354-64.

    BI-847325

    BI-847325 leads to decreased MEK expression in BRAF-mutant naïve and vemurafenib-resistant cells.  2015 Jun;14(6):1354-64.

    BI-847325

    BI-847325 inhibits growth of BRAF-mutant melanoma xenografts.  2015 Jun;14(6):1354-64.


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