1. JAK/STAT Signaling
    Stem Cell/Wnt
  2. STAT

Napabucasin 

Cat. No.: HY-13919 Purity: >98.0%
Data Sheet SDS Handling Instructions

Napabucasin is a newly found small molecule with the ability to inhibit gene transcription of STAT3, which is able to suppress cancer stemness properties and induce cell death.

For research use only. We do not sell to patients.
Napabucasin Chemical Structure

Napabucasin Chemical Structure

CAS No. : 83280-65-3

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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO $99 In-stock
5 mg $90 In-stock
10 mg $120 In-stock
50 mg $500 In-stock
100 mg $800 In-stock
200 mg   Get quote  
500 mg   Get quote  

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    Napabucasin purchased from MCE. Usage Cited in: Cancer Med. 2016 Jun;5(6):1251-8.

    Representative images of colony formation assay in PCa cell lines (PC-3 and 22RV1) and histological analysis of the colony number show that the colony formation of PCa cell lines are dramatically decreased after treated with 1 μM Napabucasin for 24 h.
    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    Napabucasin is a newly found small molecule with the ability to inhibit gene transcription of STAT3, which is able to suppress cancer stemness properties and induce cell death.

    IC50 & Target

    STAT3[1]

    In Vitro

    Napabucasin inhibits the expressions of stemness markers and kill stemness-high cancer cells isolated from several kinds of tumors except PCa. Napabucasin not only inhibits cell proliferation, cell motility, cell survival, colony formation ability, and tumorigenic potential of PCa cells, and increases cell apoptosis and sensitivity to docetaxel, but also effectively blocks sphere formation of PrCSCs and kill them as well as inhibits stemness gene expression. Napabucasin inhibits cell proliferation in PC-3 cells and 22RV1 cells at 48, 72, 96, and 120 h (P<0.05). Cell motility and colony formation ability are closely correlated with the process of tumor metastasis. Napabucasin significantly decreases colony formation and cell motility ability of PCa cell lines in vitro (P<0.05). The proliferation of PC-3 and 22RV1 cells treated with 1 μM Napabucasin are significantly decreased from day 2 to 5 compared with the control group (P<0.05)[1].

    In Vivo

    Napabucasin (40 mg/kg) or Docetaxel significantly reduces xenograft tumor growth and tumor volume (TV) compared with PBS (P<0.05). Notably, while no differences are observed between the Napabucasin and the docetaxel groups in PC-3 mouse xenograft models, the TV in Napabucasin group is even lower than docetaxel group in 22RV1 mouse xenograft models (P<0.05). Additionally, Napabucasin or docetaxel also significantly reduces tumor weight compared with PBS (P<0.05)[1].

    Clinical Trial
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    References
    Preparing Stock Solutions
    Concentration Volume Mass 1 mg 5 mg 10 mg
    1 mM 4.1630 mL 20.8151 mL 41.6302 mL
    5 mM 0.8326 mL 4.1630 mL 8.3260 mL
    10 mM 0.4163 mL 2.0815 mL 4.1630 mL
    Please refer to the solubility information to select the appropriate solvent.
    Cell Assay
    [1]

    Napabucasin is dissolved in DMSO and stored, and then diluted with appropriate media before use[1].

    The antiproliferative activity of Napabucasin against the PCa cell lines PC-3 and 22RV1 is examined. For cell proliferation assay, the PCa cell lines (22RV1 and PC-3) are seeded in 96-well plates at 2×103 cells/well in a final volume of 100 μL and incubated overnight. The proliferation of PC-3 and 22RV1 cells treated with 1 μM Napabucasin. The viability of cells is determined with CellTiter 96 non-radioactive cell proliferation assay (MTS). For colony formation assay, cells are placed in a six-well plate and maintained in RPMI-1640 supplemented with 10% FBS for 2 weeks. The colonies are fixed with 4% paraformaldehyde, stained with 0.1% crystal violet and counted[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [1]

    Napabucasin is prepared with PBS (Mice)[1].

    Mice[1]
    A total of 1×106 PC-3 cells or 8×106 22RV1 cells in 100 μL of PBS are injected subcutaneously into dorsal flanks of an immunodeficient nude mouse. The animals are treated i.p. with Napabucasin (40 mg/kg), Docetaxel (10 mg/kg), or PBS q3d once the tumors have reached 50 mm3. The tumor volume (TV) is calculated every 4 days according to the following standard formula: TV (mm3)=length×width2×0.5. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References
    Molecular Weight

    240.21

    Formula

    C₁₄H₈O₄

    CAS No.

    83280-65-3

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Shipping

    Room temperature in continental US; may vary elsewhere

    Solvent & Solubility

    10 mM in DMSO

    Napabucasin is prepared in PBS[1].

    * "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

    References

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    Product Name:
    Napabucasin
    Cat. No.:
    HY-13919
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