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ETC-159 (Synonyms: ETC-1922159)

カタログ番号GC19144

ETC-159 (ETC-1922159) は強力な経口 PORCN 阻害剤です。 ETC-159 は、β-カテニン レポーター活性を 2.9 nM の IC50 で阻害します。

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ETC-159 化学構造

Cas No.: 1638250-96-0

サイズ 価格 在庫数 個数
5mg
$45.00
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10mg
$72.00
在庫あり
50mg
$225.00
在庫あり
100mg
$405.00
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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Protocol

Cell experiment:

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].

Animal experiment:

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].

References:

[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.

Background

ETC-159 is a potent, orally available PORCN inhibitor. It inhibits β-catenin reporter activity with an IC50 of 2.9 nM.

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]

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].

References:
[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.

Chemical Properties

Cas No. 1638250-96-0 SDF
同義語 ETC-1922159
Canonical SMILES O=C(NC1=CC=C(C2=CC=CC=C2)N=N1)CN3C=NC4=C3C(N(C)C(N4C)=O)=O
Formula C19H17N7O3 M.Wt 391.38
溶解度 DMSO : ≥ 34 mg/mL (86.87 mM) Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 2.5551 mL 12.7753 mL 25.5506 mL
5 mM 0.511 mL 2.5551 mL 5.1101 mL
10 mM 0.2555 mL 1.2775 mL 2.5551 mL
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Average Rating: 5 ★★★★★ (Based on Reviews and 29 reference(s) in Google Scholar.)

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