1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEETC-159Cat. No.: HY-18988CAS No.: 1638250-96-0Synonyms: ETC-1922159分式: CHNO分量: 391.38作靶點: Wnt作通路: Stem Cell/Wnt儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數據體外實驗 DMSO : 34 mg/mL (86.87 mM)* means sol

2、uble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 2.5551 mL 12.7753 mL 25.5506 mL5 mM 0.5110 mL 2.5551 mL 5.1101 mL10 mM 0.2555 mL 1.2775 mL 2.5551 mL請根據產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。BIOLOGICAL ACTIVITY物活性 ETC-159有效的，具有服活性的 PORCN 抑制劑。抑制-catenin報告基因活性的 IC50 值為

3、2.9 nM。IC50 & Target IC50: 2.9 nM (-catenin) 1體外研究ETC-159 blocks the secretion and activity of all Wnts. ETC-159 has robust activity in multiple cancer models1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemEdriven by high Wnt signaling. ETC-159 is highly efficacious in molecularly defined colorectal

4、 cancers (CRCs)with R-spondin translocations 1體內研究 ETC-159 inhibits mouse PORCN with an IC50 of 18.1 nM, whereas the IC50 for Xenopus Porcn isapproximately four fold higher (70 nM). ETC-159 is remarkably effective in treating RSPO-translocationbearing colorectal cancer (CRC) patient-derived xenograf

5、ts. ETC-159 exhibits good oral pharmacokinetics inmice allowing preclinical evaluation via oral administration. After a single oral dose of 5 mg/kg, ETC-159 israpidly absorbed into the blood with a Tmax of 0.5 h and oral bioavailability of 100% 1.PROTOCOLCell Assay 1 HEK293 cells stably transfected

6、with STF reporter and pPGK-WNT3A plasmid (STF3A cells) are treated withvarying concentrations of compounds. For Wnt secretion, STF3A cells are treated with ETC-159 diluted in1% fetal bovine serum-containing media 1.MCE has not independently confirmed the accuracy of these methods. They are for refer

7、ence only.Animal Mice: For human xenograft models, patient-derived solid tissue fragments are subcutaneously implanted inAdministration 1 BALB/c nude mice. All groups are matched for tumor size with equal variance before treatment. ETC-159formulated in 50% PEG400 (vol/vol) in water is administered b

8、y oral gavage at a dosing volume of 10L/gbody weight 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.戶使本產品發表的科研獻 PRACTICAL ONCOLOGY JOURNAL. 2018,32(02):103-106.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Madan B, et al. Wnt addiction of genetically defined cancers reversed by PORCN inhibition. Oncogene. 2015 Aug 10. doi:10.1038/onc.2015.280.McePdfHeightCaution: Product has not been fully validated for medical applic