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Purity: ≥98%
Napabucasin (formerly also known as BBI-608; BBI608; BBI 608) is a novel, potent, and orally bioavailable cancer cell stemness inhibitor with potential antineoplastic activity. Although 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 are 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. Napabucasin was also reported to be a STAT3 inhibitor which blocks stem cell activity in cancer cells.
| ln Vitro |
Napabucasin kills high stemness cancer cells isolated from various tumors, excluding prostate cancer, and inhibits the expression of stemness markers. In addition to reducing PCa cells' capacity for colony formation, motility, survival, and tumorigenic potential, napabucasin also raises their susceptibility to docetaxel and promotes cell apoptosis. It also effectively prevents PrCSCs from forming spheroid bodies and ultimately kills them. Stemness gene expression is suppressed concurrently. PC-3 and 22RV1 cells' ability to proliferate was inhibited by napabucasin at 48, 72, 96, and 120 hours (P<0.05). The ability of cells to migrate and form colonies is intimately linked to the process of tumor metastasis. The in vitro colony formation and cell motility of PCa cell lines were significantly decreased by napabucasin (P<0.05). Day 2 to Day 5 (P<0.05) saw a significant decrease in PC-3 and 22RV1 cell proliferation when treated with 1 μM napabucasin as compared to the control group[1].
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| ln Vivo |
When compared to PBS, napabucasin (40 mg/kg) or docetaxel significantly decreased the growth and tumor volume (TV) of xenograft tumors (P<0.05). It is noteworthy that in the PC-3 mouse xenograft model, there was no discernible difference between the Napabucasin and the docetaxel groups; however, in the 22RV1 mouse xenograft model, the TV of the Napabucasin group was much lower than that of the docetaxel group. (P<0.05). Furthermore, when compared to PBS, napabucasin or docetaxel can dramatically reduce tumor weight (P<0.05)[1].
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| References |
[1]. Zhang Y, et al. Suppression of prostate cancer progression by cancer cell stemness inhibitor napabucasin. Cancer Med. 2016 Jun;5(6):1251-8
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| Molecular Formula |
C14H8O4
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| Molecular Weight |
240.21
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| CAS # |
83280-65-3
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| Related CAS # |
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| SMILES |
O=C(C1=C2OC(C(C)=O)=C1)C3=C(C2=O)C=CC=C3
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| Chemical Name |
2-Acetylnaphtho[2,3-b]furan-4,9-dione
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| Synonyms |
BBI-608; Napabucasin;BBI608; BBI 608
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.1630 mL | 20.8151 mL | 41.6302 mL | |
| 5 mM | 0.8326 mL | 4.1630 mL | 8.3260 mL | |
| 10 mM | 0.4163 mL | 2.0815 mL | 4.1630 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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