Art. -Nr.: HY-18988

ETC-159

(Synonyms: ETC-1922159)

8 Cited Publications

Kundenbewertung

Based on 8 publication(s) in Google Scholar

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.

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Reinheit: 99.13%
CAS. Nr.: 1638250-96-0
Formel: C₁₉H₁₇N₇O₃
Molecular Weight:391.38

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

ETC-159 Chemical Structure

CAS. Nr.: 1638250-96-0

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (8)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

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]

Alle Wnt Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	IC₅₀	2.9 nM Compound: ETC159	Inhibition of porcupine in human HEK293 cells assessed as reduction in Wnt secretion by measuring suppression of beta-catenin reporter activity after 24 hrs by STF reporter assay Inhibition of porcupine in human HEK293 cells assessed as reduction in Wnt secretion by measuring suppression of beta-catenin reporter activity after 24 hrs by STF reporter assay	[PMID: 26522946]
HT-1080	IC₅₀	18.1 nM Compound: ETC159	Inhibition of mouse porcupine expressed in human HT1080 cells assessed as reduction in beta catenin reporter activity using firefly luciferase substrate STF reporter assay Inhibition of mouse porcupine expressed in human HT1080 cells assessed as reduction in beta catenin reporter activity using firefly luciferase substrate STF reporter assay	[PMID: 26522946]
HT-1080	IC₅₀	70 nM Compound: ETC159	Inhibition of xenopus porcupine expressed in human HT1080 cells assessed as reduction in beta catenin reporter activity using firefly luciferase substrate STF reporter assay Inhibition of xenopus porcupine expressed in human HT1080 cells assessed as reduction in beta catenin reporter activity using firefly luciferase substrate STF reporter assay	[PMID: 26522946]

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]

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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 T_max of ~0.5 h and oral bioavailability of 100%^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 1638250-96-0
Appearance Solid
Molecular Weight 391.38
Formel C₁₉H₁₇N₇O₃
Color White to off-white
SMILES

O=C(NC1=CC=C(C2=CC=CC=C2)N=N1)CN3C=NC4=C3C(N(C)C(N4C)=O)=O
Synonyms

ETC-1922159
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (8)

All WB

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Journal Impact Factor

Sci Adv

Combinatorial screening of biochemical and physical signals for phenotypic regulation of stem cell-based cartilage tissue engineering. [Abstract]

2020 May 22;6(21):eaaz5913. PMID: 32494742
Cell Rep

Modeling human ectopic pregnancies with trophoblast and vascular organoids. [Abstract]

2023 May 23;42(6):112546. PMID: 37224015
Eur J Pharmacol

Novel PORCN inhibitor WHN-88 targets Wnt/β-catenin pathway and prevents the growth of Wnt-driven cancers. [Abstract]

2023 Apr 15:945:175628. PMID: 36858339
Sci Rep

WNT inhibition activates interferon stimulated gene expression by alleviating epigenetic repression of endogenous retroviruses. [Abstract]

2026 Mar 5. PMID: 41781472
Am J Physiol Endocrinol Metab

Amelioration of bone fragility by pulsed electromagnetic fields in type 2 diabetic KK-Ay mice involving Wnt/β-catenin signaling. [Abstract]

2021 May 1;320(5):E951-E966. PMID: 33719588
Cell Transplant

Telocyte-Derived Exosomes Provide an Important Source of Wnts That Inhibits Fibrosis and Supports Regeneration and Repair of Endometrium. [Abstract]

2023 Jan-Dec:32:9636897231212746. PMID: 38006220
Npj Viruses

The Wnt/β-catenin pathway is important for replication of SARS-CoV-2 and other pathogenic RNA viruses. [Abstract]

2024 Feb 21;2(1):6. PMID: 40295745
PRACTICAL ONCOLOGY JOURNAL

2018,32(02):103-106.

ETC-159 purchased from MedChemExpress. Usage Cited in: PRACTICAL ONCOLOGY JOURNAL. 2018,32(02):103-106.

Effects of ETC-159 on the Wnt signaling pathway in SCC-15 cells.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 50 mg/mL (127.75 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.5551 mL

12.7753 mL

25.5506 mL

5 mM

0.5110 mL

2.5551 mL

5.1101 mL

10 mM

0.2555 mL

1.2775 mL

2.5551 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (6.39 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (6.39 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Protokoll

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (276 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.5551 mL	12.7753 mL	25.5506 mL	63.8765 mL
	5 mM	0.5110 mL	2.5551 mL	5.1101 mL	12.7753 mL
	10 mM	0.2555 mL	1.2775 mL	2.5551 mL	6.3877 mL
	15 mM	0.1703 mL	0.8517 mL	1.7034 mL	4.2584 mL
	20 mM	0.1278 mL	0.6388 mL	1.2775 mL	3.1938 mL
	25 mM	0.1022 mL	0.5110 mL	1.0220 mL	2.5551 mL
	30 mM	0.0852 mL	0.4258 mL	0.8517 mL	2.1292 mL
	40 mM	0.0639 mL	0.3194 mL	0.6388 mL	1.5969 mL
	50 mM	0.0511 mL	0.2555 mL	0.5110 mL	1.2775 mL
	60 mM	0.0426 mL	0.2129 mL	0.4258 mL	1.0646 mL
	80 mM	0.0319 mL	0.1597 mL	0.3194 mL	0.7985 mL
	100 mM	0.0256 mL	0.1278 mL	0.2555 mL	0.6388 mL

Keywords

ETC-159

8 Cited Publications

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ETC-159

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

Anti-Prostate Cancer Compound Library

Anti-Pulmonary Fibrosis Compound Library

Cancer Stem Cells Compound Library

Antihypertensive Compound Library

Extracellular Vesicles (EVs) Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

Anti-Aging Compound Library Mini

MCE Bioactive Compound Library

Clinical Compound Library Plus

Bioactive Compound Library

Anti-Gastric Cancer Compound Library

Anti-Fibrosis Compound Library

High-Throughput Bioactive Compound Library

Anti-Rheumatic Arthritis Compound Library

Publications Citing Use of MedChemExpress (MCE) ETC-159

Alle Wnt Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (8)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

ETC-159

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

Anti-Prostate Cancer Compound Library

Anti-Pulmonary Fibrosis Compound Library

Cancer Stem Cells Compound Library

Antihypertensive Compound Library

Extracellular Vesicles (EVs) Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

Anti-Aging Compound Library Mini

MCE Bioactive Compound Library

Clinical Compound Library Plus

Bioactive Compound Library

Anti-Gastric Cancer Compound Library

Anti-Fibrosis Compound Library

High-Throughput Bioactive Compound Library

Anti-Rheumatic Arthritis Compound Library

Publications Citing Use of MedChemExpress (MCE) ETC-159

Alle Wnt Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (8)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

ETC-159 Related Classifications

HY-18988 Related Classifications