Home JAK/STAT STAT inhibitor Napabucasin (BBI608) For research use only.

Napabucasin (BBI608)

Synonyms: BBI608

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

Napabucasin (BBI608) Chemical Structure

Napabucasin (BBI608) Chemical Structure

CAS No. 83280-65-3

Purity & Quality Control

Napabucasin (BBI608) Related Products

Signaling Pathway

STAT Signaling Pathways

STAT Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human DU145 cells Function assay 72 h Anticancer activity against human DU145 cells after 72 hrs by XTT assay, IC50=0.02304 μM 18829316
human HaCaT cells Function assay 48 h Antihyperproliferative activity against human HaCaT cells after 48 hrs by phase contrast microscopy, IC50=0.5 μM 22845014
human HaCaT cells Proliferation assay Antiproliferative activity against human HaCaT cells, IC50=0.5 μM 10479319
KB cells Cytotoxicity assay Effective cytotoxic dose against KB cells was evaluated, ED50=4.2 μM 9873618
MDA-MB-231 Cytotoxicity assay 72 hrs Cytotoxicity against human MDA-MB-231 cells assessed as growth inhibition after 72 hrs by MTT assay, IC50 = 0.34 μM. 28558333
HepG2 Cytotoxicity assay 72 hrs Cytotoxicity against human HepG2 cells assessed as growth inhibition after 72 hrs by MTT assay, IC50 = 0.66 μM. 28558333
A549 Cytotoxicity assay 72 hrs Cytotoxicity against human A549 cells assessed as growth inhibition after 72 hrs by MTT assay, IC50 = 0.74 μM. 28558333
K562 Antiproliferative assay 48 hrs Antiproliferative activity against human K562 cells measured after 48 hrs by MTT assay, IC50 = 1 μM. 30003778
MDA-MB-231 Function assay 4 hrs Inhibition of STAT3 phosphorylation at Y705 in human MDA-MB-231 cells assessed as reduction in ratio of phosphorylated STAT3 to total STAT3 level after 4 hrs by HTRF assay, EC50 = 1.9 μM. 30003778
MDA-MB-231 Function assay 4 hrs Inhibition of STAT3 phosphorylation at Y705 in human MDA-MB-231 cells after 4 hrs by HTRF assay, EC50 = 2 μM. 30003778
MDA-MB-231 Antiproliferative assay 48 hrs Antiproliferative activity against human MDA-MB-231 cells measured after 48 hrs by MTT assay, IC50 = 2.1 μM. 30003778
HepG2 Antiproliferative assay 48 hrs Antiproliferative activity against human HepG2 cells after 48 hrs by CCK-8 assay, IC50 = 10.2 μM. 29604543
L02 Antiproliferative assay 48 hrs Antiproliferative activity against human L02 cells after 48 hrs by CCK-8 assay, IC50 = 18.7 μM. 29604543
MDA-MB-231 Function assay 100 uM 1 hr Binding affinity to STAT3 in human MDA-MB-231 cells at 100 uM treated for 1 hr followed by thermolysin addition measured after 30 mins by DARTS-Western blot analysis 30003778
MDA-MB-231 Function assay 5 umol/L 24 hrs Induction of superoxide generation in human MDA-MB-231 cells at 5 umol/L measured after 24 hrs by DHE staining based flow cytometry 30003778
MDA-MB-231 Function assay 5 umol/L 24 hrs Induction of superoxide generation in human MDA-MB-231 cells at 5 umol/L measured after 24 hrs in presence of NQO1 inhibitor dicoumarol by DHE staining based flow cytometry 30003778
Click to View More Cell Line Experimental Data

Biological Activity

Description Napabucasin (BBI608) is an orally available Stat3 and cancer cell stemness inhibitor.
Targets
Stat3 [1]
In vitro
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 Research 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.
Experimental Result Images Methods Biomarkers Images PMID
Western blot CDK4 / Cyclin D1 STAT3 / β-catenin / c-Myc c-Myc / Nanog / Bmi-1 / Axl / Sox2 / Klf4 / β-catenin / Survivin 31277685
Immunofluorescence STAT3 Cleaved caspase-3 31277685
Growth inhibition assay Cell viability 31277685
In Vivo
In vivo In mice bearing PaCa-2 xenografts, Napabucasin (20 mg/kg, i.p.) significantly inhibits tumor growth, relapse and metastasis. [1]
Animal Research Animal Models Mice bearing PaCa-2 xenografts
Dosages 20 mg/kg
Administration i.p.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03525405 Completed
ADME|Healthy
Sumitomo Pharma America Inc.
 May 18 2018 Phase 1
NCT03416816 Terminated
Neoplasms
Sumitomo Pharma America Inc.|Syneos Health
 May 15 2018 Phase 1
NCT02279719 Completed
Hepatocellular Carcinoma
Sumitomo Pharma America Inc.
 December 2014 Phase 1|Phase 2

Chemical Information & Solubility

Molecular Weight 240.21 Formula

C14H8O4
CAS No. 83280-65-3 SDF Download Napabucasin (BBI608) SDF
Smiles CC(=O)C1=CC2=C(O1)C(=O)C3=CC=CC=C3C2=O
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 14 mg/mL ( (58.28 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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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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