相关产品推荐更多 >
万千商家帮你免费找货
0 人在求购买到急需产品
- 详细信息
- 技术资料
- 保存条件:
Powder:2-8℃,2 years;Insolvent(母液):-20℃,6 months;-80℃,1 year
- 保质期:
Powder:2-8℃,2 years;Insolvent(母液):-20℃,6 months;-80℃,1 year
- 英文名:
ETC-159
- 库存:
现询
- 供应商:
北京索莱宝科技有限公司
- CAS号:
1638250-96-0
- 规格:
100mg/50mg/25mg/10mg/5mg
| 规格: | 100mg | 产品价格: | ¥4490.0 |
|---|---|---|---|
| 规格: | 50mg | 产品价格: | ¥2490.0 |
| 规格: | 25mg | 产品价格: | ¥1490.0 |
| 规格: | 10mg | 产品价格: | ¥790.0 |
| 规格: | 5mg | 产品价格: | ¥490.0 |
| 基本信息 | |
| CAS | No.1638250-96-0 |
| 英文名称 | ETC-159 |
| 分子式 | C19H17N7O3 |
| 分子量 | 391.38 |
| 溶解性 | Soluble in DMSO ≥5mg/mL(Need ultrasonic) |
| 纯度 | ≥98% |
| 外观(性状) | White to off-white Solid |
| 储存条件 | Powder:2-8℃,2 years;Insolvent(母液):-20℃,6 months;-80℃,1 year |
| MDL | MFCD29472267 |
| 靶点 | Porcupine/PORCN |
| 通路 | Stem Cells |
| 背景说明 | ETC-159是有效的 PORCN 抑制剂。 |
| 生物活性 | 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.[1] |
| IC50 | IC50: 2.9 nM (β-catenin)[1] |
| In Vitro | 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[1] |
| 细胞实验 | 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%[1]. |
| 细胞实验 | HEK293 cells stably transfected with STF reporter and pPGK-WNT3A plasmid (STF3A cells) are treated with varying concentrations of compounds. For Wnt secretion, STF3A cells are treated with ETC-159 diluted in 1% fetal bovine serum-containing media[1]. |
| 动物实验 | Mice: For human xenograft models, patient-derived solid tissue fragments are subcutaneously implanted in BALB/c nude mice. All groups are matched for tumor size with equal variance before treatment. ETC-159 formulated in 50% PEG400 (vol/vol) in water is administered by oral gavage at a dosing volume of 10?μL/g body weight[1]. |
| 数据来源文献 | [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. |
| 单位 | 瓶 |
风险提示:丁香通仅作为第三方平台,为商家信息发布提供平台空间。用户咨询产品时请注意保护个人信息及财产安全,合理判断,谨慎选购商品,商家和用户对交易行为负责。对于医疗器械类产品,请先查证核实企业经营资质和医疗器械产品注册证情况。
技术资料暂无技术资料 索取技术资料
IE3080 ETC-159 抑制剂/拮抗剂/激动剂 索莱宝
¥490 - 4490










