Napabucasin (BBI608)

Catalog No.S7977 Synonyms: BBI608

For research use only.

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

Napabucasin (BBI608) Chemical Structure

CAS No. 83280-65-3

Selleck's Napabucasin (BBI608) has been cited by 20 publications

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Biological Activity

Description Napabucasin (BBI608) 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 M3ixb2Z2dmO2aX;uJIF{e2G7 MVW3NkBp M3\rNGFvfGmlYX7j[ZIh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDEWVE1PSClZXzsd{Bi\nSncjC3NkBpenNiYomgXHRVKGG|c3H5MEBKSzVyPUCuNFI{ODRizszN NFHiRYI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOEiyPVMyPid-MUi4Nlk{OTZ:L3G+
human HaCaT cells M33qU2Z2dmO2aX;uJIF{e2G7 MoW5OFghcA>? M2DXbmFvfGmqeYDldpBzd2yrZnXyZZRqfmViYXP0bZZqfHliYXfhbY5{fCCqdX3hckBJ[UOjVDDj[YxteyCjZoTldkA1QCCqcoOgZpkheGijc3WgZ49vfHKjc4SgcYlkem:|Y3;wfUwhUUN3ME2wMlUh|ryP NG\aSo49[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Mki0OVAyPCd-MkK4OFUxOTR:L3G+
human HaCaT cells NIH5UGFRem:uaX\ldoF1cW:wIHHzd4F6 M4LiTWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSHHDZXQh[2WubIOsJGlEPTB;MD61JO69VQ>? NIX3S2U9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zMES3PVMyQSd-MUC0O|k{OTl:L3G+
KB cells M37XS2N6fG:2b4jpZ4l1gSCjc4PhfS=> NWfTe2xLTW[oZXP0bZZmKGO7dH;0c5hq[yCmb4PlJIFo[Wmwc4SgT2Ih[2WubIOge4F{KGW4YXz1ZZRm\CxiRVS1NF01NjJizszN NUjufIo2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxOUi3N|YyQCd-OUi3N|YyQDxxYU6=
MDA-MB-231 Mk\2R5l1d3SxeHnjbZR6KGG|c3H5 MYG3NkBpenN? NYXjS3NwS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVUSDLV3CMVI{OSClZXzsd{Bie3Onc4Pl[EBieyCpcn;3eIghcW6qaXLpeIlwdiCjZoTldkA4OiCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwJF0hOC5|NDFOwG0v M1vMUVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6NUW4N|M{Lz5{OEW1PFM{OzxxYU6=
HepG2 NWPEOos4S3m2b4TvfIlkcXS7IHHzd4F6 MmPMO|IhcHK| Mn;sR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gTIVxTzJiY3XscJMh[XO|ZYPz[YQh[XNiZ4Lve5RpKGmwaHnibZRqd25iYX\0[ZIhPzJiaILzJIJ6KE2WVDDhd5NigSxiSVO1NEA:KDBwNk[g{txONg>? NWiwVXpbRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMki1OVg{OzNpPkK4OVU5OzN|PD;hQi=>
A549 NYHhOJBjS3m2b4TvfIlkcXS7IHHzd4F6 M3jWPVczKGi{cx?= MYfDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDBOVQ6KGOnbHzzJIF{e2W|c3XkJIF{KGe{b4f0bEBqdmirYnn0bY9vKGGodHXyJFczKGi{czDifUBOXFRiYYPzZZktKEmFNUCgQUAxNjd2IN88UU4> M2XsXFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6NUW4N|M{Lz5{OEW1PFM{OzxxYU6=
K562 M371bmFvfGmycn;sbYZmemG2aY\lJIF{e2G7 MYe0PEBpenN? NVy5eIU3SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDLOVYzKGOnbHzzJI1m[XO3cnXkJIFnfGW{IES4JIhzeyCkeTDNWHQh[XO|YYmsJGlEPTBiPTCxJO69VS5? NYi5c212RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CwNFM4PzhpPkOwNFA{Pzd6PD;hQi=>
MDA-MB-231 MXrGeY5kfGmxbjDhd5NigQ>? MYC0JIhzew>? MlLLTY5pcWKrdHnvckBw\iCVVFHUN{BxcG:|cHjvdplt[XSrb36gZZQhYTdyNTDpckBpfW2jbjDNSGEuVUJvMkOxJINmdGy|IHHzd4V{e2WmIHHzJJJm\HWldHnvckBqdiC{YYTpc{Bw\iCyaH;zdIhwenmuYYTl[EBUXEGWMzD0c{B1d3SjbDDTWGFVOyCuZY\lcEBi\nSncjC0JIhzeyCkeTDIWHJHKGG|c3H5MEBGSzVyIE2gNU46KM7:TT6= NWXldIZpRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CwNFM4PzhpPkOwNFA{Pzd6PD;hQi=>
MDA-MB-231 MYnGeY5kfGmxbjDhd5NigQ>? NV7vfGd7PCCqcoO= MnjPTY5pcWKrdHnvckBw\iCVVFHUN{BxcG:|cHjvdplt[XSrb36gZZQhYTdyNTDpckBpfW2jbjDNSGEuVUJvMkOxJINmdGy|IHHmeIVzKDRiaILzJIJ6KEiWUl[gZZN{[XluIFXDOVAhRSB{IN88UU4> NWLnOlNFRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CwNFM4PzhpPkOwNFA{Pzd6PD;hQi=>
MDA-MB-231 NGPWTmNCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= NF34NHI1QCCqcoO= NXjaVol{SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNSGEuVUJvMkOxJINmdGy|IH3lZZN2emWmIHHmeIVzKDR6IHjyd{BjgSCPVGSgZZN{[XluIFnDOVAhRSB{LkGg{txONg>? M3eyWFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyMECzO|c5Lz5|MECwN|c4QDxxYU6=
HepG2 NEHX[mhCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= NHzUZlk1QCCqcoO= MVLBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEincFeyJINmdGy|IHHmeIVzKDR6IHjyd{BjgSCFQ1utPEBie3OjeTygTWM2OCB;IEGwMlIh|ryPLh?= MnnLQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl4MES1OFMoRjJ7NkC0OVQ{RC:jPh?=
L02 NUj0VINGSW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= MorKOFghcHK| NFfZXo1CdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFywNkBk\WyuczDh[pRmeiB2ODDodpMh[nliQ1PLMVgh[XO|YYmsJGlEPTBiPTCxPE44KM7:TT6= MkTZQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl4MES1OFMoRjJ7NkC0OVQ{RC:jPh?=
MDA-MB-231 MmPjSpVv[3Srb36gZZN{[Xl? M2GzOVExOCC3TR?= NHTPdW8yKGi{ M2DpPGJqdmSrbnegZYZncW6rdImgeI8hW1SDVEOgbY4hcHWvYX6gUWRCNU2ELUKzNUBk\WyuczDheEAyODBidV2geJJm[XSnZDDmc5IhOSCqcjDmc4xtd3enZDDifUB1cGW{bX;sfZNqdiCjZHTpeIlwdiCvZXHzeZJm\CCjZoTldkA{OCCvaX7zJIJ6KESDUmTTMXdme3Sncn6gZoxwfCCjbnHsfZNqew>? MlizQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzByMEO3O|goRjNyMECzO|c5RC:jPh?=
MDA-MB-231 M4DSbmZ2dmO2aX;uJIF{e2G7 NFL1eY42KHWvb3yvUC=> MWOyOEBpenN? MlXXTY5lfWO2aX;uJI9nKHO3cHXyc5hq\GViZ3Xu[ZJifGmxbjDpckBpfW2jbjDNSGEuVUJvMkOxJINmdGy|IHH0JFUhfW2xbD;MJI1m[XO3cnXkJIFnfGW{IEK0JIhzeyCkeTDETGUhe3SjaX7pcoch[mG|ZXSg[oxwfyCleYTvcYV1enl? NULxSXRzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CwNFM4PzhpPkOwNFA{Pzd6PD;hQi=>
MDA-MB-231 MnX4SpVv[3Srb36gZZN{[Xl? NIPERmY2KHWvb3yvUC=> M3ziW|I1KGi{cx?= NWXLXWkzUW6mdXP0bY9vKG:oIIP1dIVzd3irZHWg[4Vv\XKjdHnvckBqdiCqdX3hckBOTEFvTVKtNlMyKGOnbHzzJIF1KDVidX3vcE9NKG2nYYP1doVlKGGodHXyJFI1KGi{czDpckBxemW|ZX7j[UBw\iCQUV:xJIlvcGmkaYTvdkBlcWOxdX3hdo9tKGK7IFTISUB{fGGrbnnu[{Bj[XOnZDDmcI94KGO7dH;t[ZRzgQ>? M1PlSlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyMECzO|c5Lz5|MECwN|c4QDxxYU6=
Assay
Methods Test Index PMID
Western blot CDK4 / Cyclin D1 ; STAT3 / β-catenin / c-Myc ; c-Myc / Nanog / Bmi-1 / Axl / Sox2 / Klf4 / β-catenin / Survivin 31277685 25605917
Immunofluorescence STAT3 ; Cleaved caspase-3 31277685
Growth inhibition assay Cell viability 31277685
In vivo In mice bearing PaCa-2 xenografts, Napabucasin (20 mg/kg, i.p.) significantly inhibits tumor growth, relapse and metastasis. [1]

Protocol (from reference)

Cell Research:

[1]

  • 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]

  • 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.

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 3 years -20°C powder
2 years -80°C in solvent
Smiles CC(=O)C1=CC2=C(O1)C(=O)C3=CC=CC=C3C2=O

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

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% DMSO % % Tween 80 % ddH2O
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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

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 Terminated Drug: DSP-0337 Neoplasms Sumitomo Dainippon Pharma Oncology Inc|Syneos Health May 15 2018 Phase 1
NCT02279719 Completed Drug: BBI608|Drug: BBI503|Drug: Sorafenib Hepatocellular Carcinoma Sumitomo Dainippon Pharma Oncology Inc December 2014 Phase 1|Phase 2

(data from https://clinicaltrials.gov, updated on 2022-01-17)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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