ETC-159

製品コードS6616 バッチS661601

印刷

化学情報

Synonyms

ETC-1922159

Storage
(From the date of receipt)

3 years -20°C powder

化学式

C₁₉H₁₇N₇O₃

分子量

391.38

CAS No.

1638250-96-0

Solubility (25°C)*

体外

DMSO

78 mg/mL (199.29 mM)

Water

Insoluble

Ethanol

Insoluble

体内（毎回新しく調製した物を用意してください）

Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 Corn oil この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	1.500mg/ml (3.83mM)	Taking the 1 mL working solution as an example, add 50 μL of 30 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	ETC-159 (ETC-1922159) は、STF3A細胞におけるβ-カテニンレポーター活性を阻害するIC50が2.9 nMの経口投与可能な強力なporcupine阻害剤です。
in vitro	ETC-159 treatment causes decreased abundance of Wnt3a-stabilized β-catenin protein in both mouse L cells and HEK293 cells. This compound inhibits β-catenin signaling in response to multiple active Wnts. It inhibits mouse PORCN with an IC50 of 18.1 nM, whereas the IC50 for Xenopus Porcn is approximately fourfold higher (70 nM).
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 mg/kg in mice, this compound is rapidly absorbed into the blood with a Tmax of ~0.5 h and oral bioavailability of 100%. The plasma half-life is ~1.18 h and its concentration in the blood remained above the in vitro IC50 for at least 16 h. Treatment of mice with increasing doses of this chemical leads to a dose-related increase in exposure. It also effectively inhibits Wnt autocrine signaling and growth of teratocarcinomas. This compound 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 this chemical in genetically defined tumors induces irreversible cellular differentiation thus preventing regrowth of these tumors.

プロトコル(参考用のみ)

細胞アッセイ	細胞株	Mouse L cells
	濃度	100 nM
	反応時間	0-24 h
	実験の流れ	Mouse L cells stably expressing Wnt3a are trypsinizised and treated with DMSO or 100 nM ETC-159 before plating in cell culture dishes. The cells are harvested at indicated time points and total β-catenin levels are assessed by immunoblot.
動物実験	動物モデル	BALB/c nude, NCr nude or NOD-scid-gamma mice
	投薬量	5, 30 or 100 mg/kg
	投与方法	by oral gavage

参考

https://pubmed.ncbi.nlm.nih.gov/26257057/

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Molecular mechanisms of tubulogenesis revealed in the sea star hydro-vascular organ [ Nat Commun, 2023, 14(1):2402]	PubMed: 37160908
Characterization of RNF43 frameshift mutations that drive Wnt ligand- and R-spondin-dependent colon cancer [ J Pathol, 2022, 10.1002/path.5868]	PubMed: 35040131

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。