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ETC-159 is a potent, selective and orally available PORCN inhibitor, which inhibits β-catenin reporter activity with an IC50 of 2.9 nM. 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 remarkably effective in treating RSPO-translocation bearing colorectal cancer (CRC) patient-derived xenografts. 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 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%
| Cell Experiment | |
|---|---|
| Cell lines | HEK293 cells, STF3A cells |
| Preparation method | 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. |
| Concentrations | 100 nm |
| Incubation time | 24 h |
| Animal Experiment | |
|---|---|
| Animal models | Mice |
| Formulation | Formulated in 50% PEG400 (vol/vol) in water |
| Dosages | 10 μL/g |
| Administration | oral gavage |
| Molecular Weight | 391.38 |
| Formula | C19H17N7O3 |
| CAS Number | 1638250-96-0 |
| Solubility (25°C) | DMSO: ≥ 25 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Wnt/beta-catenin Products |
|---|
| XAV939
XAV939 is a potent, cell-permeable small molecule inhibitor of the Wnt/β-catenin pathway to TNKS1 and TNKS2 with IC50 values of 11 and 4 nM respectively. |
| ICG-001
ICG-001 is a novel small molecule inhibitor of TCF/beta-catenin-mediated transcription. ICG-001 specifically binds to cyclic AMP response element-binding protein with an IC50 of 3 μM. |
| IWP-2
IWP-2 is an inhibitor of Wnt production that impairs Wnt pathway activity in vitro with an IC50 value of 27 nM. |
| IWP-L6
IWP-L6 is a highly potent Porcn inhibitor with EC50 of 0.5 nM. |
| IWR-1-endo
IWR-1 (endo-IWR 1) is a Wnt pathway inhibitor with IC50 of 180 nM, induces Axin2 protein levels and promotes β-catenin phosphorylation by stabilizing Axin-scaffolded destruction complexes. |
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Products are for research use only. Not for human use. We do not sell to patients.
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