ETC-159 (Synonyms: ETC-1922159) |
| Catalog No.GC19144 |
ETC-159(ETC-1922159)는 강력한 경구용 PORCN 억제제입니다. ETC-159는 2.9nM의 IC50으로 β-카테닌 리포터 활성을 억제합니다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1638250-96-0
Sample solution is provided at 25 µL, 10mM.
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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.
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. | |
| Cas No. | 1638250-96-0 | SDF | |
| Synonyms | 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 |
| Solubility | 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. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
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 |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 29 reference(s) in Google Scholar.)
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