Network Version
ETC-159 Data Sheet
| Product Name: | ETC-159 |
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|---|---|---|
| CAS No.: | 1638250-96-0 | |
| Cat. No.: | HY-18988 | |
| MWt: | 391.38 | |
| Formula: | C19H17N7O3 | |
| Purity : | >98% | |
| Solubility: | DMSO : 50 mg/mL (127.75 mM; Need ultrasonic) | |
| Mechanisms: | Target: Cancer | |
| Biological Activity: | ||
| 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] 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]. | ||
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