ETC-159

1638250-96-0

C19H17N7O3

DMSO : >= 34 mg/mL (86.87 mM)

Stem Cell/Wnt

ETC-159 is a potent, orally available PORCN inhibitor. It inhibits beta-catenin reporter activity with an IC₅₀ of 2.9 nM. IC50 & Target: IC50: 2.9 nM (beta-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 T_max of ca.0.5 h and oral bioavailability of 100%^[1].