ETC-159

Catalog No.S6616 Synonyms: ETC-1922159

For research use only.

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

CAS No. 1638250-96-0

Selleck's ETC-159 has been cited by 1 Publication

Purity & Quality Control

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

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].

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].

Protocol (from reference)

Cell Research:

[1]

  • 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.

Animal Research:

[1]

  • Animal Models: BALB/c nude, NCr nude or NOD-scid-gamma mice
  • Dosages: 5, 30 or 100 mg/kg
  • Administration: by oral gavage

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 391.38
Formula

C19H17N7O3

CAS No. 1638250-96-0
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CN1C2=C(C(=O)N(C1=O)C)N(C=N2)CC(=O)NC3=NN=C(C=C3)C4=CC=CC=C4

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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02521844 Recruiting Drug: ETC-1922159|Drug: Pembrolizumab Solid Tumors EDDC (Experimental Drug Development Centre) A*STAR Research Entities|PPD October 2015 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-08-01)

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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