1. Stem Cell/Wnt
  2. Wnt

ETC-159 (Synonyms: ETC-1922159)

Cat. No.: HY-18988 Purity: 98.39%
Data Sheet SDS Handling Instructions

ETC-159 is a potent, orally available PORCN inhibitor. It 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

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO $110 In-stock
5 mg $100 In-stock
10 mg $150 In-stock
50 mg $440 In-stock
100 mg $660 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Description

ETC-159 is a potent, orally available PORCN inhibitor. It 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]

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].

Clinical Trial
NCT Number Sponsor Condition Start Date Phase
NCT02521844 D3 (Drug Discovery and Development), Biomedical Sciences Institute|PPD Solid Tumors October 2015 Phase 1
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References
Preparing Stock Solutions
Concentration Volume (DMSO) 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
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]

Mouse: 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
M.Wt

391.38

Formula

C₁₉H₁₇N₇O₃

CAS No.

1638250-96-0

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO: ≥ 34 mg/mL

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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Product Name:
ETC-159
Cat. No.:
HY-18988
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