中文名：ETC-159
英文名：ETC-159
纯度：Moligand™，≥98%
货号：E413550
Cas号：1638250-96-0
存储温度：-20°C储存
运输条件：超低温运输
产品介绍：
Information
ETC-159 ETC-159 (ETC-1922159) is an orally available, potent porcupine inhibitor with an IC50 of 2.9 nM for inhibiting β-catenin reporter activity in STF3A cells.
Targets
Porcn
In vitro
ETC-159 treatment causes decreased abundance of Wnt3a-stabilized β-catenin protein in both mouse L cells and HEK293 cells. ETC-159 inhibits β-catenin signaling in response to multiple active Wnts. ETC-159 inhibits mouse PORCN with an IC50 of 18.1\u2009nM, whereas the IC50 for Xenopus Porcn is approximately fourfold higher (70\u2009nM).
In vivo
ETC-159 is orally bioavailable and effectively inhibits the growth of mouse mammary tumor virus-Wnt1 tumors. After a single oral dose of 5\u2009mg/kg in mice, ETC-159 is rapidly absorbed into the blood with a Tmax of ~0.5\u2009h and oral bioavailability of 100%. The plasma half-life is ~1.18\u2009h and its concentration in the blood remained above the in vitro IC50 for at least 16\u2009h. Treatment of mice with increasing doses of ETC-159 leads to a dose-related increase in exposure. ETC-159 also effectively inhibits Wnt autocrine signaling and growth of teratocarcinomas. ETC-159 effectively inhibits the growth and induces differentiation of colon cancers with RSPO translocations and induces global remodeling of gene expression. Suppression of Wnt/β-catenin signaling with ETC-159 in genetically defined tumors induces irreversible cellular differentiation thus preventing regrowth of these tumors.
Cell Research(from reference)
Cell lines：Mouse L cells
Concentrations：100\u2009nM
Incubation Time：0-24 h
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关键字： 1,2,3,6-四氢-1,3-二甲基-2,6-二氧代-N-(6-苯基-3-哒嗪基)-7H-嘌呤-7-乙酰胺;NSC809251 ; NSC-809251 ; 2-(1,3-Dimethyl-2,6-dioxo-1,2,3,6-tetrahydro-7H-purin-7-yl)-N-(6-phenylpyridazin-3-yl)acetamide
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