Napabucasin (BBI608)

Cas：83280-65-3

Product Information：

Napabucasin, also known as BBI-608, is an orally available cancer cell stemness inhibitor with potential antineoplastic activity. Even though the exact target has yet to be fully elucidated, BBI608 appears to target and inhibit multiple pathways involved in cancer cell stemness. This may ultimately inhibit cancer stemness cell (CSC) growth as well as heterogeneous cancer cell growth. CSCs, self-replicating cells that are able to differentiate into heterogeneous cancer cells, appear to be responsible for the malignant growth, recurrence and resistance to conventional chemotherapies.

Chemical Formula: C14H8O4

Exact Mass: 240.0423

Molecular Weight: 240.214

Elemental Analysis: C, 70.00; H, 3.36; O, 26.64

Synonym: 

BBI608

BBI 608

BB-I608

Napabucasin

Chemical Name:  

2-Acetylnaphtho[2,3-b]furan-4,9-dione

InChi Key:

DPHUWDIXHNQOSY-UHFFFAOYSA-N

InChi Code:   InChI=1S/C14H8O4/c1-7(15)11-6-10-12(16)8-4-2-3-5-9(8)13(17)14(10)18-11/h2-6H,1H3

Smiles Code:

O=C(C1=C2OC(C(C)=O)=C1)C3=C(C2=O)C=CC=C3

Technical Data：

Appearance: Yellow solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

In Vitro：

Napabucasin inhibits the expressions of stemness markers and kill stemness-high cancer cells isolated from several kinds of tumors except PCa.

Napabucasin not only inhibits cell proliferation, cell motility, cell survival, colony formation ability, and tumorigenic potential of PCa cells, and increases cell apoptosis and sensitivity to docetaxel, but also effectively blocks sphere formation of PrCSCs and kill them as well as inhibits stemness gene expression.

Napabucasin inhibits cell proliferation in PC-3 cells and 22RV1 cells at 48, 72, 96, and 120 h (P<0.05). Cell motility and colony formation ability are closely correlated with the process of tumor metastasis.

Napabucasin significantly decreases colony formation and cell motility ability of PCa cell lines in vitro (P<0.05). The proliferation of PC-3 and 22RV1 cells treated with 1 μM Napabucasin are significantly decreased from day 2 to 5 compared with the control group (P<0.05).

In Vivo：

Napabucasin (40 mg/kg) or Docetaxel significantly reduces xenograft tumor growth and tumor volume (TV) compared with PBS (P<0.05). Notably, while no differences are observed between the Napabucasin and the docetaxel groups in PC-3 mouse xenograft models, the TV in Napabucasin group is even lower than docetaxel group in 22RV1 mouse xenograft models (P<0.05). Additionally, Napabucasin or docetaxel also significantly reduces tumor weight compared with PBS (P<0.05).

References：

1. Zhang Y, Jin Z, Zhou H, Ou X, Xu Y, Li H, Liu C, Li B. Suppression of prostate cancer progression by cancer cell stemness inhibitor napabucasin. Cancer Med. 2016 Feb 21. doi: 10.1002/cam4.675. [Epub ahead of print] PubMed PMID: 26899963.

2. Li Y, Rogoff HA, Keates S, Gao Y, Murikipudi S, Mikule K, Leggett D, Li W, Pardee AB, Li CJ. Suppression of cancer relapse and metastasis by inhibiting cancer stemness. Proc Natl Acad Sci U S A. 2015 Feb 10;112(6):1839-44. doi: 10.1073/pnas.1424171112. Epub 2015 Jan 20. PubMed PMID: 25605917; PubMed Central PMCID: PMC4330785.

Products are for research use only. Not for human use.