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。

ETC-159 (ETC-1922159) is a potent, orally available PORCN inhibitor. ETC-159 inhibits β-catenin reporter activity with an IC 50 of 2.9 nM.

Solid

IC50: 2.9 nM (β-catenin)

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 has not independently confirmed the accuracy of these methods. They are for reference only.

ETC-159 inhibits mouse PORCN with an IC 50 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%. has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[1]. Madan B, et al. Wnt addiction of genetically defined cancers reversed by PORCN inhibition. Oncogene. 2015 Aug 10. doi: 10.1038/onc.2015.280.

In Vitro: DMSO : 50 mg/mL (127.75 mM; Need ultrasonic)配制储备液