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Description: ETC-159 (ETC-192215) is a novel, potent and orally bioavailable PORCN inhibitor which inhibits beta-catenin reporter activity with an IC50 of 2.9 nM and 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. ETC-159 is remarkably effective in treating RSPO-translocation bearing colorectal cancer (CRC) patient-derived xenografts.
References: Oncogene. 2016 Apr 28; 35(17):2197-207.
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