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    Napabucasin (BBI-608)
    Napabucasin (BBI-608)

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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 #: V1386
    CAS #: 83280-65-3Purity ≥98%

    Description: Napabucasin (formerly also known as BBI-608; BBI608; BBI 608) is a novel, potent, and orally bioavailable cancer cell stemness inhibitor with potential antineoplastic activity. Although the exact target has yet to be fully elucidated, BBI608 appears to target and inhibit multiple pathways involved in cancer cell stemness. This may ultimately inhibit cancer stemness cell (CSC) growth as well as heterogeneous cancer cell growth. CSCs are self-replicating cells that are able to differentiate into heterogeneous cancer cells, appear to be responsible for the malignant growth, recurrence and resistance to conventional chemotherapies. Napabucasin was also reported to be a STAT3 inhibitor which blocks stem cell activity in cancer cells.

    References: Proc Natl Acad Sci U S A. 2015 Feb 10;112(6):1839-44.

    Publications Citing Use of InvivoChem Napabucasin (BBI-608)J Exp Clin Cancer Res. 2021 Oct 13;40(1):319. doi: 10.1186/s13046-021-02117-z

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    Molecular Weight (MW)240.21
    CAS No.83280-65-3
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 10 mg/mL (41.6 mM)
    Water: <1 mg/mL
    Ethanol: <1 mg/mL
    Solubility (In vivo)5% DMSO+corn oil: 1 mg/mL
    Other infoSynonym: BBI-608; Napabucasin; BBI608; BBI 608
    Chemical Name: 2-Acetylnaphtho[2,3-b]furan-4,9-dione
    SMILES Code: O=C(C1=C2OC(C(C)=O)=C1)C3=C(C2=O)C=CC=C3

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    In Vitro

    In vitro activity: Napabucasin downregulates stemness gene expression driven by Stat3 and cancer stemness properties, and effectively inhibits self-renewal of stemness-high cancer cells with IC50 ranged from 0.291~1.19 μM, on inhibition on normal stem cells.

    Cell Assay: For cancer stem cells (U87-MG, U118, COLO205, DLD1, SW480, HCT116, FaDu, ACHN, SNU-475, Huh7, HepG2, H1975, A549, H460, CAOV-3, SW-626, PaCa2.) spheres are dissociated and plated under cancer stem cell culture conditions on coated 96-well plates. After 72 h of culture, wells are dosed with the indicated compounds. Seventy-two hours or 24 h after dosing, CellTiter-Glo 2.0 is added to each well, and the luminescence is measured as described by the manufacturer. IC50 values are calculated by fitting a four parameter dose–response curve to normalized data using GraphPad Prism software. For bulk cells, cells are plated at 5,000 cells per well on 96-well plates. Twenty-four hours after plating, cells are treated with the indicated compounds. Viability is determined at 72 h as described above.

    In VivoIn mice bearing PaCa-2 xenografts, Napabucasin (20 mg/kg, i.p.) significantly inhibits tumor growth, relapse and metastasis.
    Animal modelmice bearing PaCa-2 xenografts
    Formulation & Dosage20 mg/kg; i.p. injection
    ReferencesProc Natl Acad Sci U S A. 2015 Feb 10;112(6):1839-44

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


    Inhibition of cancer relapse by BBI608. Proc Natl Acad Sci U S A. 2015 Feb 10;112(6):1839-44.


    Comparison between BBI608 and current cancer therapeutics. Proc Natl Acad Sci U S A. 2015 Feb 10;112(6):1839-44.


    Inhibition of self-renewal of stemness-high cancer cells by BBI608. Proc Natl Acad Sci U S A. 2015 Feb 10;112(6):1839-44.


    Depletion of stemness-high cancer cells by BBI608 in vivo. Proc Natl Acad Sci U S A. 2015 Feb 10;112(6):1839-44.


    BBI608 inhibits stemness gene expression. Proc Natl Acad Sci U S A. 2015 Feb 10;112(6):1839-44.



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