ETC-159 (Synonyms: ETC-1922159)

Name: ETC-159
Brand: MedChemExpress
SKU: HY-18988
Rating: 5.0 (8 reviews)

Cat. No.: HY-18988 Purity: 98.96%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

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.

For research use only. We do not sell to patients.

ETC-159 Chemical Structure

CAS No. : 1638250-96-0

Size	Price	Stock	Quantity

Free Sample (0.1 - 0.5 mg)		Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 61	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 61	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 55	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 88	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 165	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 275	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 495	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 8 publication(s) in Google Scholar

7 Publications Citing Use of MCE ETC-159

•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.

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Biological Activity
Protocol
Purity & Documentation
References
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Description

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]

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

Molecular Weight

391.38

Formula

C₁₉H₁₇N₇O₃

CAS No.

1638250-96-0

Appearance

Solid

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

View the Complete Stock Solution Preparation Table

* 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.

Molarity Calculator
Dilution Calculator

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

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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

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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 98.96%

Select Batch:

Data Sheet (275 KB) SDS (251 KB)

COA (250 KB) HNMR (137 KB) LCMS (94 KB)

Handling Instructions (2659 KB)

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. [Content Brief]

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]. 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]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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. [Content Brief]

Complete Stock Solution Preparation Table

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

ETC-159 Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

ETC-1591638250-96-0ETC-1922159ETC159ETC 159ETC1922159ETC 1922159PorcupineWntInhibitorinhibitorinhibit

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ETC-159 (Synonyms: ETC-1922159)

Customer Review

ETC-159 Related Antibodies

7 Publications Citing Use of MCE ETC-159

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Complete Stock Solution Preparation Table

ETC-159 Related Classifications

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