Napabucasin (BBI608)

Catalog No.S7977 Batch:S797701

Technical Data

Formula	C₁₄H₈O₄
Molecular Weight	240.21	CAS No.	83280-65-3
Solubility (25°C)*	In vitro	DMSO	10 mg/mL (41.63 mM)
		Water	Insoluble
		Ethanol	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * 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. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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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]

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 Assay:^{^[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.
Animal Study:^{^[1]}	Animal Models Mice bearing PaCa-2 xenografts Dosages 20 mg/kg Administration i.p.

Cell Assay:^{^[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.

Animal Study:^{^[1]}

Animal Models
Mice bearing PaCa-2 xenografts
Dosages
20 mg/kg
Administration
i.p.

References

[1] Li Y, et al. Proc Natl Acad Sci U S A. 2015, 112(6), 1839-1844.

Selleck's Napabucasin (BBI608) has been cited by 29 publications

Serum amyloid A promotes glycolysis of neutrophils during PD-1 blockade resistance in hepatocellular carcinoma [ Nat Commun, 2024, 15(1):1754]	PubMed: 38409200
Molecular crosstalk between MUC1 and STAT3 influences the anti-proliferative effect of Napabucasin in epithelial cancers [ Sci Rep, 2024, 14(1):3178]	PubMed: 38326371
ADAR1-mediated RNA editing of SCD1 drives drug resistance and self-renewal in gastric cancer [ Nat Commun, 2023, 14(1):2861]	PubMed: 37208334
Targeting VCP potentiates immune checkpoint therapy for colorectal cancer [ Cell Rep, 2023, 42(11):113318]	PubMed: 37865914
Alcohol reshapes a liver premetastatic niche for cancer by extra- and intrahepatic crosstalk-mediated immune evasion [ Mol Ther, 2023, 31(9):2662-2680]	PubMed: 37469143
Prolonging lung cancer response to EGFR inhibition by targeting the selective advantage of resistant cells [ BioRxiv, 2023, 10.1101/2023.06.19.545595]	PubMed: none
CRISPRi screens in human iPSC-derived astrocytes elucidate regulators of distinct inflammatory reactive states [ Nat Neurosci, 2022, 25(11):1528-1542]	PubMed: 36303069
Ligand-mediated PAI-1 inhibition in a mouse model of peritoneal carcinomatosis [ Cell Rep Med, 2022, 3(2):100526]	PubMed: 35243423
Targeted inhibition of STAT3 induces immunogenic cell death of hepatocellular carcinoma cells via glycolysis [ Mol Oncol, 2022, 16(15):2861-2880]	PubMed: 35665592
Identification of Novel Therapeutic Targets for Fibrolamellar Carcinoma Using Patient Derived Xenografts and Direct from Patient Screening [ Cancer Discov, 2021, candisc.0872.2020]	PubMed: 34127480

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SHIPPING AND STORAGE
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