ETC-159

Synonyms: ETC-1922159

ETC-159 (ETC-1922159) is an orally available, potent porcupine inhibitor with an IC50 of 2.9 nM for inhibiting β-catenin reporter activity in STF3A cells.

ETC-159 Chemical Structure

ETC-159 Chemical Structure

CAS: 1638250-96-0

Selleck's ETC-159 has been cited by 2 publications

Purity & Quality Control

Batch: Purity: 99.88%
99.88

ETC-159 Related Products

Choose Selective PORCN Inhibitors

Biological Activity

Description ETC-159 (ETC-1922159) is an orally available, potent porcupine inhibitor with an IC50 of 2.9 nM for inhibiting β-catenin reporter activity in STF3A cells.
Targets
Porcn [1]
In vitro
In vitro

ETC-159 treatment causes decreased abundance of Wnt3a-stabilized β-catenin protein in both mouse L cells and HEK293 cells. ETC-159 inhibits β-catenin signaling in response to multiple active Wnts. ETC-159 inhibits mouse PORCN with an IC50 of 18.1 nM, whereas the IC50 for Xenopus Porcn is approximately fourfold higher (70 nM)[1].

Cell Research Cell lines Mouse L cells
Concentrations 100 nM
Incubation Time 0-24 h
Method

Mouse L cells stably expressing Wnt3a are trypsinizised and treated with DMSO or 100 nM ETC-159 before plating in cell culture dishes. The cells are harvested at indicated time points and total β-catenin levels are assessed by immunoblot.

In Vivo
In vivo

ETC-159 is orally bioavailable and effectively inhibits the growth of mouse mammary tumor virus-Wnt1 tumors. After a single oral dose of 5 mg/kg in mice, ETC-159 is rapidly absorbed into the blood with a Tmax of ~0.5 h and oral bioavailability of 100%. The plasma half-life is ~1.18 h and its concentration in the blood remained above the in vitro IC50 for at least 16 h. Treatment of mice with increasing doses of ETC-159 leads to a dose-related increase in exposure. ETC-159 also effectively inhibits Wnt autocrine signaling and growth of teratocarcinomas. ETC-159 effectively inhibits the growth and induces differentiation of colon cancers with RSPO translocations and induces global remodeling of gene expression. Suppression of Wnt/β-catenin signaling with ETC-159 in genetically defined tumors induces irreversible cellular differentiation thus preventing regrowth of these tumors[1].

Animal Research Animal Models BALB/c nude, NCr nude or NOD-scid-gamma mice
Dosages 5, 30 or 100 mg/kg
Administration by oral gavage
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02521844 Active not recruiting
Solid Tumors
EDDC (Experimental Drug Development Centre) A*STAR Research Entities|PPD
October 2015 Phase 1

Chemical Information & Solubility

Molecular Weight 391.38 Formula

C19H17N7O3

CAS No. 1638250-96-0 SDF --
Smiles CN1C2=C(C(=O)N(C1=O)C)N(C=N2)CC(=O)NC3=NN=C(C=C3)C4=CC=CC=C4
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 78 mg/mL ( (199.29 mM); Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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