| 產(chǎn)品描述： | LF3是β-Catenin/TCF4相互作用的拮抗劑，具有抗腫瘤活性。IC50值為1.65 μM。 |
| 靶點(diǎn)： |
IC50: 1.65 μM (β-Catenin/TCF4, AlphaScreen), 1.82 μM (β-Catenin/TCF4, ELISA);Wnt/beta-catenin |
| 體外研究： |
LF3 inhibits Wnt/β-catenin signals in cells with exogenous reporters and in colon cancer cells with endogenously high Wnt activity. LF3 also suppresses features of cancer cells related to Wnt signaling, including high cell motility, cell-cycle progression, and the overexpression of Wnt target genes. However, LF3 does not cause cell death or interfere with cadherin-mediated cell-cell adhesion. Remarkably, the self-renewal capacity of cancer stem cells is blocked by LF3 in concentration-dependent manners. |
| 體內(nèi)研究： |
LF3 reduces tumor growth and induces differentiation in a mouse xenograft model of colon cancer. Tumor growth is significantly reduced when mice with GFPhigh cells are treated with LF3 at 50 mg/kg. LF3 treatment does not disturb the normal histology of the gut of mice. |
| 參考文獻(xiàn)： |
1. Fang L, et al. A Small-Molecule Antagonist of the β-Catenin/TCF4 Interaction Blocks the Self-Renewal of Cancer Stem Cells and Suppresses Tumorigenesis. Cancer Res. 2016 Feb 15;76(4):891-901. |
| 溶解性： |
Soluble in DMSO |
| 保存條件： |
-20℃ |
| 配置溶液濃度參考： |
|
1mg |
5mg |
10mg |
| 1 mM |
2.401 ml |
12.003 ml |
24.006 ml |
| 5 mM |
0.48 ml |
2.401 ml |
4.801 ml |
| 10 mM |
0.24 ml |
1.2 ml |
2.401 ml |
| 50 mM |
0.048 ml |
0.24 ml |
0.48 ml |
|
| 注意： |
部分產(chǎn)品我司僅能提供部分信息，我司不保證所提供信息的權(quán)威性，僅供客戶參考交流研究之用。 |
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