化学信息：
| 化学名 | 2-(1,3-dimethyl-2,6-dioxopurin-7-yl)-N-(6-phenylpyridazin-3-yl)acetamide |
|
| 简称 | ETC-159 | |
| 别名 |
SCHEMBL17626176, UNII-5L854240DQ, 5L854240DQ, CS-5162, ETC-1922159 |
|
| 中文名 | N/A | |
| 化学式 | C19H17N7O3 | |
| 分子量 | 391.38 | |
| CAS号 | 1638250-96-0 | |
| 纯度 | 98% | |
| 溶剂/溶解度 |
Water<1mg/ml; DMSO34mg/ml; Ethanol<1mg/ml |
|
| 溶液配制 | 5mg加入1.28ml DMSO，或者每3.91mg加入1ml DMSO，配制成10mM溶液。SF6813-10mM用DMSO配制。 |
生物信息：
| 产品描述 | ETC-159 is a potent and specific inhibitor of Wnt secretion. ETC-159 inhibits β-catenin reporter activity in a dose-dependent manner with an IC50 of 2.9nM. | ||||
| 信号通路 | Stem Cells & Wnt | ||||
| 靶点 | Wnt | － | － | － | － |
| IC50 | 2.9nM | － | － | － | － |
| 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 18.1nM, whereas the IC50for Xenopus Porcn was approximately fourfold higher (70nM). 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 5mg/kg, ETC-159 is rapidly absorbed into the blood with a Tmax of ~0.5h and oral bioavailability of 100%. | ||||
| 临床实验 | N/A | ||||
| 特征 | N/A | ||||
相关实验数据(此数据来自于公开文献，碧云天并不保证其有效性)：
| 酶活性检测实验 | |
| 方法 | N/A |
| 细胞实验 | |
| 细胞系 | N/A |
| 浓度 | N/A |
| 处理时间 | N/A |
| 方法 | N/A |
| 动物实验 | |
| 动物模型 | N/A |
| 配制 | N/A |
| 剂量 | N/A |
| 给药方式 | N/A |
| 产品编号 | 产品名称 | 包装 |
| SF6813-10mM | ETC-159 (Wnt抑制剂) | 10mM×0.2ml |
| SF6813-5mg | ETC-159 (Wnt抑制剂) | 5mg |
| SF6813-25mg | ETC-159 (Wnt抑制剂) | 25mg |
| — | 说明书 | 1份 |
保存条件：
-20℃保存，至少一年有效。5mg和25mg包装也可室温保存，至少6个月有效。如果溶于非DMSO溶剂，建议分装后-80℃保存，预计6个月内有效。
