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ETC-159 (Synonyms: ETC-1922159) 纯度: ≥98.0%
ETC-159 (ETC-1922159) 是有效的,具有口服活性的 PORCN 抑制剂。抑制β-catenin报告基因活性的 IC50 值为2.9 nM。
ETC-159 Chemical Structure
CAS No. : 1638250-96-0
规格 | 价格 | 是否有货 | 数量 |
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Free Sample (0.1-0.5 mg) | Apply now | ||
10 mM * 1 mL in DMSO | ¥550 | In-stock | |
5 mg | ¥500 | In-stock | |
10 mg | ¥800 | In-stock | |
25 mg | ¥1500 | In-stock | |
50 mg | ¥2500 | In-stock | |
100 mg | ¥4500 | In-stock | |
200 mg | 询价 | ||
500 mg | 询价 |
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ETC-159 相关产品
•相关化合物库:
- Clinical Compound Library Plus
- Bioactive Compound Library Plus
- Stem Cell Signaling Compound Library
- Wnt/Hedgehog/Notch Compound Library
- Anti-Cancer Compound Library
- Clinical Compound Library
- Anti-Aging Compound Library
- Differentiation Inducing Compound Library
- Cytoskeleton Compound Library
- Orally Active Compound Library
- Neuroprotective Compound Library
- Anti-Breast Cancer Compound Library
- Anti-Liver Cancer Compound Library
- Anti-Colorectal Cancer Compound Library
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. |
IC50 & Target |
IC50: 2.9 nM (β-catenin)[1] |
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体外研究 (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] 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
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体内研究 (In Vivo) |
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]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
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Clinical Trial |
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分子量 |
391.38 |
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Formula |
C19H17N7O3 |
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CAS 号 |
1638250-96-0 |
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运输条件 |
Room temperature in continental US; may vary elsewhere. |
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储存方式 |
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溶解性数据 |
In Vitro:
DMSO : 50 mg/mL (127.75 mM; Need ultrasonic) 配制储备液
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请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 In Vivo:
请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
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参考文献 |
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Cell Assay [1] |
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]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
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Animal Administration [1] |
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]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
参考文献 |
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