ETC-159CAS号: 1638250-96-0分子式: C19H17N7O3分子量: 391.38描述纯度储存/保存方法别名外观可溶性/溶解性靶点In vitro(体外研究)In vivo(体内研究)
产品描述 | |
描述 |
ETC-159 is a potent and specific inhibitor of Wnt secretion. ETC-159 inhibits _beta_-catenin reporter activity in a dose-dependent manner with an IC50 of 2.9 nM.
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纯度 |
>98%
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储存/保存方法 |
Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.
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基本信息 | |
别名 |
ETC 159,ETC159,ETC 1922159,ETC-1922159,ETC1922159
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外观 |
Powder
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可溶性/溶解性 |
DMSO: ≥ 34 mg/mL
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生物活性 | |
靶点 |
Wnt
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In vitro(体外研究) |
ETC-159 blocks the secretion and activity of all Wnts. ETC-159 has robust activity in multiple cancer models driven by high Wnt signaling. ETC-159 is highly efficacious in molecularly defined colorectal cancers (CRCs) with R-spondin translocations
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In vivo(体内研究) |
ETC-159 inhibits mouse PORCN with an IC50 of 18.1 nM, whereas the IC50 for Xenopus Porcn is approximately four fold higher (70 nM). ETC-159 is remarkably effective in treating RSPO-translocation bearing colorectal cancer (CRC) patient-derived xenografts. ETC-159 exhibits good oral pharmacokinetics in mice allowing preclinical evaluation via oral administration. After a single oral dose of 5 mg/kg, ETC-159 is rapidly JPorbed into the blood with a Tmax of ~0.5 h and oral bioavailability of 100%.
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分子结构图