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].
Fields:
ETC-159 is a potent and specific inhibitor of Wnt secretion. ETC-159 inhibits _beta_-catenin reporter activity in a dose-dependent manner with an IC50 of 2.9 nM.
Specificity:
Target: Wnt . Fields: ETC-159 is a potent and specific inhibitor of Wnt secretion. ETC-159 inhibits _beta_-catenin reporter activity in a dose-dependent manner with an IC50 of 2.9 nM.
Source:
Rabbit
Dilution:
IC50: 2.9 nM (β-catenin)[1]
Concentration:
>98%
Storage Stability:
2 years -20°C Powder, 2 weeks4°C in DMSO,6 months-80°C in DMSO