1. Stem Cell/Wnt
  2. Porcupine
    Wnt
  3. ETC-159

ETC-159 (Synonyms: ETC-1922159)

Cat. No.: HY-18988 Purity: 98.67%
Handling Instructions

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

ETC-159 Chemical Structure

CAS No. : 1638250-96-0

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Free Sample (0.5-1 mg)   Apply Now  
10 mM * 1 mL in DMSO USD 55 In-stock
Estimated Time of Arrival: December 31
5 mg USD 50 In-stock
Estimated Time of Arrival: December 31
10 mg USD 80 In-stock
Estimated Time of Arrival: December 31
25 mg USD 150 In-stock
Estimated Time of Arrival: December 31
50 mg USD 250 In-stock
Estimated Time of Arrival: December 31
100 mg USD 450 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 3 publication(s) in Google Scholar

Top Publications Citing Use of Products

    ETC-159 purchased from MCE. Usage Cited in: PRACTICAL ONCOLOGY JOURNAL. 2018,32(02):103-106.

    Effects of ETC-159 on the Wnt signaling pathway in SCC-15 cells.
    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    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]

    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]

    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 Tmax of ~0.5 h and oral bioavailability of 100%[1].

    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

    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 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 50 mg/mL (127.75 mM; Need ultrasonic)

    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
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 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

    • 2.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.5 mg/mL (6.39 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    References
    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
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    Keywords:

    ETC-159ETC-1922159ETC159ETC 159ETC1922159ETC 1922159PorcupineWntInhibitorinhibitorinhibit

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    Product Name:
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    Cat. No.:
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