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作靶點(diǎn): -catenin作通路: Stem Cell/Wnt儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 32 mg/mL (76.82 mM)* means soluble, but saturatio

2、n unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液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請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存式和期限。體內(nèi)實(shí)驗(yàn)請根據(jù)您的實(shí)驗(yàn)動物和給藥式選擇適當(dāng)?shù)娜芙獍?，配制前請先配制澄清的儲備液，再依次添加助溶?為保證實(shí)驗(yàn)結(jié)果的可靠性，體內(nèi)實(shí)驗(yàn)的作液，建議您現(xiàn)現(xiàn)配，當(dāng)天使；澄清的儲備液可以根據(jù)儲存條件，

3、適當(dāng)保存；以下溶劑前的百分 指該溶劑在您配制終溶液中的體積占)：1. 請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (6.00 mM); Clear solution2. 請依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (6.00 mM); Clear solution3. 請依序添加每種溶劑： 10% DMSO 90% corn oil1/2 Master of Small Molecules 您邊的抑

4、制劑師www.MedChemESolubility: 2.5 mg/mL (6.00 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 LF3-Catenin/TCF4相互作的拮抗劑，具有抗腫瘤活性。IC50值為1.65 M。IC50 & Target IC50: 1.65 M (-Catenin/TCF4, AlphaScreen), 1.82 M (-Catenin/TCF4, ELISA) 1體外研究 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.體內(nèi)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.戶使本產(chǎn)品發(fā)表的科研獻(xiàn) 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 您邊的抑制劑師www.MedChemECaution: Product has not been fully