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- 详细信息
- 文献和实验
- 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 |
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文献和实验the probe stay for 1.5 hrs RT for complete erythrocyte lysis Count platelets under a phase contrast microscope at x400 magnification using Neubauer hemocytometer SOLUTIONS The Unopette Reservoir
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the probe stay for 1.5 hrs RT for complete erythrocyte lysis Count platelets under a phase contrast microscope at x400 magnification using Neubauer hemocytometer SOLUTIONS The Unopette Reservoir
物质(例如,海藻生体毒素)[48]。全细胞生物传感器可以检测污染物中生物片段(例如,片段可以进入活体细胞并激活特定的反应途径),可以获得以其它分析技术很难获得的环境和毒物学的相关信息。基于BL重组全细胞的检测方法同样可以应用到药物筛选中,可以检测待筛选药物与药物靶点的特异性结合。例如,通过监测报告基因的激活状态可以评估激动剂和对抗剂。这些检测方法为功能性检测,可以在一定的生物学背景中测量待筛选药物在特定胞内途径中的作用,而不是获得简单的结合证据。 同一细胞内可以使用两个报告基因可以单独表达并单独
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