ETC-159

Catalog No.S6616 Batch:S661602

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Technical Data

Formula

C19H17N7O3
Molecular Weight 391.38 CAS No. 1638250-96-0
Solubility (25°C)* In vitro DMSO 78 mg/mL (199.29 mM)
Water Insoluble
Ethanol Insoluble
* <1 mg/ml means slightly soluble or 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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 Assay:

[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 Study:

[1]
  • Animal Models

    BALB/c nude, NCr nude or NOD-scid-gamma mice

  • Dosages

    5, 30 or 100 mg/kg

  • Administration

    by oral gavage

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

Molecular mechanisms of tubulogenesis revealed in the sea star hydro-vascular organ [ Nat Commun, 2023, 14(1):2402] PubMed: 37160908
Characterization of RNF43 frameshift mutations that drive Wnt ligand- and R-spondin-dependent colon cancer [ J Pathol, 2022, 10.1002/path.5868] PubMed: 35040131

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.