Napabucasin

Catalog No.S7977 Synonyms: BBI608

Napabucasin Chemical Structure

Molecular Weight(MW): 240.21

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

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Biological Activity

Description Napabucasin is an orally available Stat3 and cancer cell stemness inhibitor.
Targets
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 Ml;mSpVv[3Srb36gZZN{[Xl? NUn2TGNLPzJiaB?= NYnCd3VUSW62aXPhcoNmeiCjY4Tpeol1gSCjZ3HpcpN1KGi3bXHuJGRWOTR3IHPlcIx{KGGodHXyJFczKGi{czDifUBZXFRiYYPzZZktKEmFNUC9NE4xOjNyNDFOwG0> M3LoblE5QDJ7M{G2
human HaCaT cells NUfGeXJQTnWwY4Tpc44h[XO|YYm= MmnwOFghcA>? M1:5b2FvfGmqeYDldpBzd2yrZnXyZZRqfmViYXP0bZZqfHliYXfhbY5{fCCqdX3hckBJ[UOjVDDj[YxteyCjZoTldkA1QCCqcoOgZpkheGijc3WgZ49vfHKjc4SgcYlkem:|Y3;wfUwhUUN3ME2wMlUh|ryP NUPZbIhOOjJ6NEWwNVQ>
human HaCaT cells NFT3dIhRem:uaX\ldoF1cW:wIHHzd4F6 MYXBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEijQ3HUJINmdGy|LDDJR|UxRTBwNTFOwG0> MUOxNFQ4QTNzOR?=
KB cells MUfDfZRwfG:6aXRCpIF{e2G7 NX2wXJBnTW[oZXP0bZZmKGO7dH;0c5hq[yCmb4PlJIFo[Wmwc4SgT2Ih[2WubIOge4F{KGW4YXz1ZZRm\CxiRVS1NF01NjJizszN NVThbmpkQTh5M{[xPC=>

... Click to View More Cell Line Experimental Data

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

Protocol

Cell Research:

[1]

+ Expand
  • 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:

[1]

+ Expand
  • Animal Models: Mice bearing PaCa-2 xenografts
  • Formulation: --
  • 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.
1mg/mL

* 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
Formula

C14H8O4

CAS No. 83280-65-3
Storage powder
in solvent
Synonyms BBI608

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03411122 Completed Drug-drug Interactions Boston Biomedical Inc June 30 2017 Phase 1
NCT03525405 Recruiting ADME|Healthy Boston Biomedical Inc May 2018 Phase 1
NCT02993731 Recruiting Carcinoma Pancreatic Ductal Boston Biomedical Inc December 2016 Phase 3
NCT02826161 Terminated Carcinoma Non-Small-Cell Lung Boston Biomedical Inc November 2016 Phase 3
NCT02851004 Recruiting Metastatic Colorectal Cancer Takayuki Yoshino|Sumitomo Dainippon Pharma Co. Ltd.|National Cancer Center Hospital East October 2016 Phase 1|Phase 2
NCT02753127 Recruiting Colorectal Cancer Boston Biomedical Inc June 2016 Phase 3

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID