| 货号 | 规格 | 价格 | 上海 | 北京 | 珠海 | 重庆 | 武汉 | 购买数量 |
|---|---|---|---|---|---|---|---|---|
S83776-5mg买3赠1 |
98.80% | ￥370.00 |
5 | - | - | - | - |
|
S83776-10mg买3赠1 |
98.80% | ￥600.00 |
6 | - | - | - | - |
|
S83776-25mg买3赠1 |
98.80% | ￥900.00 |
4 | - | - | - | - |
|
S83776-100mg促销 |
98.80% | ￥2600.00 ￥2080.00 |
2 | - | - | - | - |
|
| 产品描述： | ETC-159 (ETC-1922159) is a potent, orally available PORCN inhibitor. ETC-159 inhibits β-catenin reporter activity with an IC50 of 2.9 nM | ||||||||||||||||||||
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| 靶点： | IC50: 2.9 nM (β-catenin);Wnt/beta-catenin; Porcupine | ||||||||||||||||||||
| 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。 | ||||||||||||||||||||
| 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 absorbed into the blood with a Tmax of ~0.5 h and oral bioavailability of 100%。 | ||||||||||||||||||||
| 参考文献： | 1. Madan B, et al. Wnt addiction of genetically defined cancers reversed by PORCN inhibition. Oncogene. 2015 Aug 10. doi: 10.1038/onc.2015.280. | ||||||||||||||||||||
| 溶解性： | Soluble in DMSO | ||||||||||||||||||||
| 保存条件： | -20℃ | ||||||||||||||||||||
| 配置溶液浓度参考： |
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| 注意： | 部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
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