ETC-159

For research use only.

Catalog No.S6616 Synonyms: ETC-1922159

ETC-159 Chemical Structure

CAS No. 1638250-96-0

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.

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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

Cell Research:

[1]

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  • 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.


    (Only for Reference)
Animal Research:

[1]

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

Solubility (25°C)

In vitro DMSO 78 mg/mL (199.29 mM)
Water Insoluble
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 391.38
Formula

C19H17N7O3

CAS No. 1638250-96-0
Storage powder
in solvent
Synonyms ETC-1922159
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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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.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID