Napabucasin (BBI608)

Catalog No.S7977 Batch:S797703

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Technical Data

Formula

C14H8O4
Molecular Weight 240.21 CAS No. 83280-65-3
Solubility (25°C)* In vitro DMSO 12 mg/mL (49.95 mM)
Water Insoluble
Ethanol Insoluble
In vivo (Add solvents to the product individually and in order)
Clear solution
10%DMSO 40%PEG300 5%Tween80 45%ddH2O
0.25mg/ml Taking the 1 mL working solution as an example, add 100 μL of 2.5 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 450 μL of ddH2O to make it clear. Volume up to 1 mL. The mixed solution should be used immediately for optimal results. 
* <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.)

Preparing Stock Solutions

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.

Selleck's Napabucasin (BBI608) has been cited by 27 publications

Serum amyloid A promotes glycolysis of neutrophils during PD-1 blockade resistance in hepatocellular carcinoma [ Nat Commun, 2024, 15(1):1754] PubMed: 38409200
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
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
Exploring transcriptional regulators Ref-1 and STAT3 as therapeutic targets in malignant peripheral nerve sheath tumours [ Br J Cancer, 2021, 10.1038/s41416-021-01270-8] PubMed: 33658640
Targeting EphA2 suppresses hepatocellular carcinoma initiation and progression by dual inhibition of JAK1/STAT3 and AKT signaling [ Cell Rep, 2021, 34(8):108765] PubMed: 33626345

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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