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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 |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
| Molecular Weight | 391.38 |
| Formula | C19H17N7O3 |
| CAS Number | 1638250-96-0 |
| Purity | 99.47% |
| Solubility | DMSO: ≥ 25 mg/mL |
| Storage | at -20°C |
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