For research use only.

Catalog No.S7977 Synonyms: BBI608

8 publications

Napabucasin(BBI608) Chemical Structure

CAS No. 83280-65-3

Napabucasin (BBI608) is an orally available Stat3 and cancer cell stemness inhibitor.

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Biological Activity

Description Napabucasin (BBI608) is an orally available Stat3 and cancer cell stemness inhibitor.
Stat3 [1]
In vitro

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. [1]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human DU145 cells MXnGeY5kfGmxbjDhd5NigQ>? MYW3NkBp MnjaRY51cWOjbnPldkBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFTVNVQ2KGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDYWHQh[XO|YYmsJGlEPTB;MD6wNlMxPCEQvF2= MlzHNVg5Ojl|MU[=
human HaCaT cells NGruUWhHfW6ldHnvckBie3OjeR?= Mo\xOFghcA>? NVfw[IF4SW62aXj5dIVzeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEijQ3HUJINmdGy|IHHmeIVzKDR6IHjyd{BjgSCyaHHz[UBkd262cnHzeEBucWO{b4Pjc5B6NCCLQ{WwQVAvPSEQvF2= MlvLNlI5PDVyMUS=
human HaCaT cells MWHQdo9tcW[ncnH0bY9vKGG|c3H5 M{CzU2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSHHDZXQh[2WubIOsJGlEPTB;MD61JO69VQ>? NWn3dJVjOTB2N{mzNVk>
KB cells MmHLR5l1d3SxeHnjxsBie3OjeR?= NIC3RlZG\m[nY4TpeoUh[3m2b4TvfIlkKGSxc3WgZYdicW6|dDDLRkBk\WyuczD3ZZMh\X[jbIXheIVlNCCHREWwQVQvOiEQvF2= Mn:yPVg4OzZzOB?=

... Click to View More Cell Line Experimental Data

Methods Test Index PMID
Western blot
CDK4 / Cyclin D1; 

PubMed: 31277685     

U87MG and LN229 cells were treated with the vehicle or 5 μM Napabucasin for 48 h. Then, cell lysates were analyzed by western blotting.

STAT3 / β-catenin / c-Myc; 

PubMed: 31277685     

GSCs (glioma stem cells) under the indicated conditions were harvested and subjected to western blotting. 

c-Myc / Nanog / Bmi-1 / Axl / Sox2 / Klf4 / β-catenin / Survivin; 

PubMed: 25605917     

FaDu cancer stem cells were treated for 3, 6, or 24 h with BBI608 at either 1 or 2 μM or with DMSO (0). Cell lysates from these treated cells were then analyzed by Western blotting. BBI608 down-regulates a number of stemness related proteins involved in t䲧疝Ỵ疞㧀疜膉痘 瘿�෋ᾰƌ෋à 㺣痖帉痖Ѐ瑖堘𢡄빢᎒

31277685 25605917

PubMed: 31277685     

IF was used to estimate the expression of STAT3 in U87MG and LN229 cells after treatment with Napabucasin (scale bar: 50 μm).

Cleaved caspase-3 ; 

PubMed: 31277685     

Immunofluorescence staining of glioma cells treated with the vehicle or Napabucasin. Nuclei were stained with DAPI (blue). Scale bar = 50 μm.

Growth inhibition assay
Cell viability ; 

PubMed: 31277685     

Proliferation of glioma cells treated with Napabucasin and detected by CCK-8 assays. Half maximal inhibitory concentrations (IC50) of Napabucasin in U87MG and LN229 cells were 6.4 and 5.6 μM respectively. 

In vivo In mice bearing PaCa-2 xenografts, Napabucasin (20 mg/kg, i.p.) significantly inhibits tumor growth, relapse and metastasis. [1]


Cell Research:


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  • Cell lines: Cancer stem cells U87-MG, U118, COLO205, DLD1, SW480, HCT116, FaDu, ACHN, SNU-475, Huh7, HepG2, H1975, A549, H460, CAOV-3, SW-626, PaCa2.
  • Concentrations: ~2 μM
  • Incubation Time: 72 h
  • Method:

    For cancer stem cells, 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.

    (Only for Reference)
Animal Research:


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  • Animal Models: Mice bearing PaCa-2 xenografts
  • Dosages: 20 mg/kg
  • Administration: i.p.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 10 mg/mL (41.63 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
5% DMSO+40% PEG 300+5% Tween 80+ddH2O
For best results, use promptly after mixing.

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 240.21


CAS No. 83280-65-3
Storage powder
in solvent
Synonyms BBI608
Smiles CC(=O)C1=CC2=C(O1)C(=O)C3=CC=CC=C3C2=O

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03525405 Completed Drug: napabucasin ADME|Healthy Sumitomo Dainippon Pharma Oncology Inc May 18 2018 Phase 1
NCT03416816 Recruiting Drug: DSP-0337 Neoplasms Sumitomo Dainippon Pharma Oncology Inc|Syneos Health May 15 2018 Phase 1

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID