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ETC-159

CAS No. : 1638250-96-0

MCE 国际站：ETC-159

产品活性：ETC-159 (ETC-1922159) 是有效的，具有口服活性的 PORCN 抑制剂。抑制β-catenin报告基因活性的 IC₅₀ 值为2.9 nM。

研究领域：Stem Cell/Wnt

作用靶点：Porcupine  |  Wnt

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 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 ~0.5 h and oral bioavailability of 100%.

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