2016年1月7日星期四

ETC-159|ETC159|ETC-1922159|DC Chemicals

ETC-159|ETC159|ETC-1922159|DC Chemicals

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.

Product Name: ETC-159 |Catalog Number: DC8489 |CAS 1638250-96-0 |Other names: ETC-159,ETC 159,ETC159,ETC 1922159,ETC-1922159,ETC1922159 |Chemical Name:  |Molecule Formular: C19H17N7O3 |MW: 391.38

ETC-159 is a potent and specific inhibitor of Wnt secretion. ETC-159 inhibits β-catenin reporter activity in a dose-dependent manner with an IC50 of 2.9 nM.
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.
in vivo: ETC-159 inhibits mouse PORCN with an IC50 of 18.1 nM, whereas the IC50 for Xenopus Porcn was approximately fourfold 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%.

For research and scientific purpose only, not for human use.

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