产品说明书
ETC-159
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同义名 : | ETC-1922159 |
| CAS号 : | 1638250-96-0 | |
| 货号 : | A644611 | |
| 分子式 : | C19H17N7O3 | |
| 纯度 : | 99%+ | |
| 分子量 : | 391.383 | |
| MDL号 : | MFCD29472267 | |
| 存储条件： |
粉末 Sealed in dry,Store in freezer, under -20°C 液体 -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 50 mg/mL(127.75 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO |
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| 动物实验配方： |
| 生物活性 | |||
|---|---|---|---|
| 描述 | ETC-159 is a novel potent PORCN inhibitor with IC50 value of 2.9nM for inhibition of β-catenin reporter activity. It blocks the secretion and activity of all Wnts. It effectively inhibited the secretion of WNT3A into culture media at 100nM, but did not inhibit β-catenin signaling in STF cells supplemented with Wnt3A-conditioned medium. ETC-159 at 100nM treatment also caused decreased abundance of Wnt3a-stabilizedβ-catenin protein in both mouse L cells and HEK293 cells post 6-24h. ETC-159 inhibited the growth of mouse mammary tumor virus (MMTV)-Wnt1 tumors orally administrated with ETC-159 at 1, 3 and 10mg/kg. Similar effect of tumor growth inhibition by ETC-159 could be observed on athymic nude mice bearing PA-1 or NCCIT xenografts. Also it was remarkably effective in treating RSPO-translocation bearing colorectal cancer (CRC) patient-derived xenografts. Inhibition of PORCN by ETC-159 in RSPO3-translocated cancers causes a marked remodeling of the transcriptome, with loss of cell cycle, stem cell and proliferation genes, and an increase in differentiation markers[4]. Bones of mice treated with ETC-159 at doses of 3, 10 and 30mg/kg had loss-of-bone volume and density within 4 weeks of exposure[5]. | ||
| 作用机制 | ETC-159 potently inhibited PORCN, palmitoleation activity of which is essential for Wnts for their secretion and binding to the Frizzled receptors.[4] | ||
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
2.56mL 0.51mL 0.26mL |
12.78mL 2.56mL 1.28mL |
25.55mL 5.11mL 2.56mL |
| 参考文献 |
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