product name Napabucasin
Description: Napabucasin, also known as BBI-608, is a potent, 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.
References: Proc Natl Acad Sci U S A. 2015 Feb 10;112(6):1839-44.
240.21
Formula
C14H8O4
CAS No.
83280-65-3
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 10 mg/mL (41.6 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)
5% DMSO+corn oil: 1 mg/mL
Synonyms
BBI-608
other peoduct :
| In Vitro |
In vitro activity: 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. Kinase Assay: Cell Assay: For cancer stem cells (U87-MG, U118, COLO205, DLD1, SW480, HCT116, FaDu, ACHN, SNU-475, Huh7, HepG2, H1975, A549, H460, CAOV-3, SW-626, PaCa2.) 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. |
|---|---|
| In Vivo | In mice bearing PaCa-2 xenografts, Napabucasin (20 mg/kg, i.p.) significantly inhibits tumor growth, relapse and metastasis. |
| Animal model | mice bearing PaCa-2 xenografts |
| Formulation & Dosage | 20 mg/kg; i.p. injection |
| References | Proc Natl Acad Sci U S A. 2015 Feb 10;112(6):1839-44 |
