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    Navitoclax (ABT-263)
    Navitoclax (ABT-263)

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    InvivoChem目录号 #: V0003
    CAS号码 #: 923564-51-6纯度 ≥98%

    Description: Navitoclax (formerly ABT-263) is a novel, highly potent, orally bioavailable small-molecule inhibitor of the BCL (B-cell leukemia) protein family such as Bcl-xL, Bcl-2 and Bcl-w with Ki of ~ 0.5 nM, ~1 nM and ~1 nM in cell-free assays. It has potential anticancer activity and is currently undergoing Phase studies for the treatment of both solid and liquid tumors. ABT-263 mimicks the Bad-like BH3 and binds to Bcl-2 family proteins Bcl-2, Bcl-xl and Bcl-w which disrupts the interaction between Bcl-2/Bcl-xl /Bcl-w and pro-apoptotic proteins such as Bim(Bcl-2-interacting mediator of cell death), Bad (Bcl-2-associated death promoter) and Bak(BCL2-antagonist/killer 1), eventually it will trigger the caspases-initiated cell death pathway to induce apoptosis.

    References:  Cancer Res. 2008, 68(9), 3421-428.; Clin Cancer Res, 2008, 14(11), 3268-77.


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    Molecular Weight (MW)974.61
    FormulaC47H55ClF3N5O6S3
    CAS No.923564-51-6
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 100 mg/mL (102.6 mM)
    Water: <1 mg/mL (slightly soluble or insoluble)
    Ethanol: <1 mg/mL
    Solubility (In vivo)55% DMSO+Corn oil: 8mg/mL
    SynonymsNavitoclax; ABT 263; ABT-263; ABT263
    SMILES CodeO=C(NS(=O)(C1=CC=C(N[C@H](CCN2CCOCC2)CSC3=CC=CC=C3)C(S(=O)(C(F)(F)F)=O)=C1)=O)C4=CC=C(N5CCN(CC6=C(C7=CC=C(Cl)C=C7)CCC(C)(C)C6)CC5)C=C4


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    GeneralWhen ABT-263 is administered at 100 mg/kg/day in the H345 xenograft model, significant antitumor efficacy is observed with 80% TGI and 20% of treated tumors indicating at least a 50% reduction in tumor volume.
    Animal modelC.B -17 scid-bg or C.B -17 scid mice
    FormulationFormulated in 10% ethanol, 30% polyethylene glycol 400, and 60% Phosal 50 PG
    Dosages100 mg/kg/day
    AdministrationOral gavage
    ReferenceCancer Res. 2008, 68(9), 3421-428.; Clin Cancer Res, 2008, 14(11), 3268-77.


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

    ABT-263 (Navitoclax)

    ABT-737, or ABT-263 at the indicated doses for 24 hours. Survival data are shown for transitional B cells (n = 3 mice for each genotype) and are the results of 3 independent experiments, each performed in triplicate. Experiments depicted in panels C and D were performed concurrently. Values represent mean ± SEM.
     

    ABT-263 (Navitoclax)

     

    ABT-263 (Navitoclax)

    As an inhibitor of Bcl-2, ABT263 is effective to reduce cell viability in HG3-CLL cells. Incubating the cells with ABT263 in 96 well plates (3×104 cells per well) for 24h shows a dose-dependent inhibition of cell viability with EC50 value of 2μM.


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