ETC-159, also known as ETC-1922159, is a potent, selective and orally available PORCN inhibitor. ETC-159 blocks the secretion and activity of all Wnts. ETC-159 is remarkably effective in treating RSPO-translocation bearing colorectal cancer (CRC) patient-derived xenografts. Inhibition of Wnt signaling by PORCN inhibition holds promise as differentiation therapy in genetically defined human cancers. Enhanced sensitivity to Wnts is an emerging hallmark of a subset of cancers, defined in part by mutations regulating the abundance of their receptors
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化学信息
名称 | ETC-159 |
Iupac 化学名称 | 1,3-dimethyl-7-((6-phenylpyridazin-3-yl)glycyl)-3,4,5,7-tetrahydro-1H-purine-2,6-dione |
同义词 | ETC 159; ETC-1922159 |
英文同义词 | ETC 159; ETC-1922159 |
分子式 | C19H19N7O3 |
分子量 | 393.407 |
Smile | CN1C(N(C2N=CN(C2C1=O)C(CNC=1N=NC(=CC1)C1=CC=CC=C1)=O)C)=O |
InChiKey | COEZTQWWLJCBEC-UHFFFAOYSA-N |
InChi | InChI=1S/C19H19N7O3/c1-24-17-16(18(28)25(2)19(24)29)26(11-21-17)15(27)10-20-14-9-8-13(22-23-14)12-6-4-3-5-7-12/h3-9,11,16-17H,10H2,1-2H3,(H,20,23) |
Cas号 | 1638250-96-0 |
相关CAS号 | |
外观性状 | Solid powder |
纯度 | 98% by HPLC |
存储 | -20 ºC for 3 years |
可溶性 | Soluble in DMSO |
处理方式 | |
运输条件 | Shipped under ambient temperature |
海关编码 | |
Targets | |
Mechanism | |
Cell study | |
Animal study | |
Clinical study | |