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In vitro: LF3 does not cause cell death or interfere with cadherin-mediated cell-cell adhesion. The self-renewal capacity of cancer stem cells is blocked by LF3 in concentration-dependent manners, as examined by sphere formation of colon and head and neck cancer stem cells under nonadherent conditions. LF3 inhibits Wnt/β-catenin signaling, but does not interfere with E-cadherin/β-catenin-mediated cell-cell adhesion. LF3 blocks the expression of a series of Wnt target genes in Wnt-addicted colon cancer cells. It inhibits proliferation of Wnt-addicted colon cancer cells through induction of cell-cycle arrest and also inhibits self-renewal capacity of CSCs. In vivo: LF3 reduces tumor growth and induces differentiation in a mouse xenograft model of colon cancer while exhibiting no significant toxicity for mice and does not disturb the normal histology of the gut of mice.
| Cell Experiment | |
|---|---|
| Cell lines | The cell lines HCT116, HCT15, HT29, SW480, SW620, LS174T, SW48, MCF7, HeLa, HEK293, and MDCK |
| Preparation method | β-catenin is immunoprecipitated from protein extracts of the cells that are incubated with LF3 at increasing concentrations, and reduced TCF4 and LEF1 bound to β-catenin are shown by Western blotting. |
| Concentrations | 3.3-60 μmol/L |
| Incubation time | 24 h |
| Animal Experiment | |
|---|---|
| Animal models | NOD/SCID mice |
| Formulation | |
| Dosages | 50 mg/kg |
| Administration | i.v. |
| Molecular Weight | 416.56 |
| Formula | C20H24N4O2S2 |
| CAS Number | 664969-54-4 |
| Solubility (25°C) | 63 mg/mL in DMSO |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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