LF3 _β-catenin Antagonist - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemELF3Cat. No.: HY-101486CAS No.: 664969-54-4分式: CHNOS分量: 416.56作靶点: -catenin作通路: Stem Cell/Wnt储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 32 mg/mL (76.82 mM)* means soluble, but saturatio

2、n unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.4006 mL 12.0031 mL 24.0061 mL5 mM 0.4801 mL 2.4006 mL 4.8012 mL10 mM 0.2401 mL 1.2003 mL 2.4006 mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。体内实验请根据您的实验动物和给药式选择适当的溶解案，配制前请先配制澄清的储备液，再依次添加助溶剂(为保证实验结果的可靠性，体内实验的作液，建议您现现配，当天使；澄清的储备液可以根据储存条件，

3、适当保存；以下溶剂前的百分 指该溶剂在您配制终溶液中的体积占)：1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (6.00 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (6.00 mM); Clear solution3. 请依序添加每种溶剂： 10% DMSO 90% corn oil1/2 Master of Small Molecules 您边的抑

4、制剂师www.MedChemESolubility: 2.5 mg/mL (6.00 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 LF3-Catenin/TCF4相互作的拮抗剂，具有抗肿瘤活性。IC50值为1.65 M。IC50 & Target IC50: 1.65 M (-Catenin/TCF4, AlphaScreen), 1.82 M (-Catenin/TCF4, ELISA) 1体外研究 LF3 inhibits Wnt/-catenin signals in cells with exogenous reporters and in co

5、lon cancer cells withendogenously 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, LF3does not cause cell death or interfere with cadherin-mediated cell-

6、cell adhesion. Remarkably, the self-renewal capacity of cancer stem cells is blocked by LF3 in concentration-dependent manners 1.体内研究 LF3 reduces tumor growth and induces differentiation in a mouse xenograft model of colon cancer. Tumorgrowth is significantly reduced when mice with GFPhigh cells are

7、 treated with LF3 at 50 mg/kg. LF3treatment does not disturb the normal histology of the gut of mice 1.PROTOCOLCell Assay 1 LF3 is dissolved in DMSO to a concentration of 50 mM and diluted with culture medium. Two colon cancercell lines (HCT116 and HT29) and a breast cancer cell line (MCF7) are trea

8、ted with LF3 (0, 30, 60 M) for 24hours and labeled with BrdUrd for 4 to 5 hours to detect proliferating cells 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Mice: Unsorted GFPlow and GFPhigh SW480 cells are subcutaneously injected into the bac

9、k skin ofAdministration 1 NOD/SCID mice. Tumor growth is monitored over a period of 45 days. For therapy, LF3 is administered i.v. at50 mg/kg body weight for three rounds over 5 consecutive days, with 2-day breaks 1.MCE has not independently confirmed the accuracy of these methods. They are for refe

10、rence only.户使本产品发表的科研献 Biochem Biophys Res Commun. 2019 Aug 27;516(3):819-824.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Fang L, et al. A Small-Molecule Antagonist of the -Catenin/TCF4 Interaction Blocks the Self-Renewal of Cancer Stem Cells andSuppresses Tumorigenesis. Cancer Res. 2016 Feb 15;76(4):891-901.McePdfHeight2/2 Master of Small Molecules 您边的抑制剂师www.MedChemECaution: Product has not been fully