XAV-939

製品コードS1180 バッチS118007

印刷

化学情報

Synonyms

NVP-XAV939

Storage
(From the date of receipt)

3 years -20°C powder
1 years -80°C in solvent

化学式

C₁₄H₁₁F₃N₂OS

分子量

312.31

CAS No.

284028-89-3

Solubility (25°C)*

体外

DMSO

12 mg/mL (38.42 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	4%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。	1.000mg/ml (3.20mM)	Taking the 1 mL working solution as an example, add 40 μL of 25 mg/ml clear DMSO stock solution to 960 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	XAV-939 (NVP-XAV939) selectively inhibits Wnt/β-catenin-mediated transcription through tankyrase1/2 inhibition with IC50 of 11 nM/4 nM in cell-free assays, regulates axin levels and does not affect CRE, NF-κB or TGF-β.
in vitro	XAV-939 specifically inhibits tankyrase PARP activity. This compound dramatically decreases DNA-PKcs protein levels, confirming the critical role of tankyrase poly-ADP-ribosylation activity in maintaining stability of the DNA-PKcs protein. The greatest reduction of DNA-PKcs protein levels (< 25% relative expression compared to DMSO treated controls) occurs at 12 hours with 1.0 μM exposure. Treatment of human lymphoblasts with 1.0 μM this chemical results in marked elevation of tankyrase 1 levels. ^[1] This agent is axin stabilizing agent. It stimulates beta-catenin degradation by stabilizing axin, the concentration-limiting component of the destruction complex. This compound stabilizes axin by blocking the poly-ADP-ribosylating enzymes tankyrase 1 and tankyrase 2. Both tankyrase isoforms interact with a highly conserved domain of axin and stimulate its degradation through the ubiquitin-proteasome pathway. This chemical deregulates the Wnt/b-catenin pathway which has been implicated in many cancers. ^[2]
in vivo	XAV-939 (NVP-XAV939) selectively inhibits Wnt/β-catenin-mediated transcription through tankyrase1/2 inhibition.

製品説明

XAV-939 (NVP-XAV939) selectively inhibits Wnt/β-catenin-mediated transcription through tankyrase1/2 inhibition with IC50 of 11 nM/4 nM in cell-free assays, regulates axin levels and does not affect CRE, NF-κB or TGF-β.

in vitro

XAV-939 specifically inhibits tankyrase PARP activity. This compound dramatically decreases DNA-PKcs protein levels, confirming the critical role of tankyrase poly-ADP-ribosylation activity in maintaining stability of the DNA-PKcs protein. The greatest reduction of DNA-PKcs protein levels (< 25% relative expression compared to DMSO treated controls) occurs at 12 hours with 1.0 μM exposure. Treatment of human lymphoblasts with 1.0 μM this chemical results in marked elevation of tankyrase 1 levels. ^[1]

This agent is axin stabilizing agent. It stimulates beta-catenin degradation by stabilizing axin, the concentration-limiting component of the destruction complex. This compound stabilizes axin by blocking the poly-ADP-ribosylating enzymes tankyrase 1 and tankyrase 2. Both tankyrase isoforms interact with a highly conserved domain of axin and stimulate its degradation through the ubiquitin-proteasome pathway. This chemical deregulates the Wnt/b-catenin pathway which has been implicated in many cancers. ^[2]

in vivo

XAV-939 (NVP-XAV939) selectively inhibits Wnt/β-catenin-mediated transcription through tankyrase1/2 inhibition.

プロトコル(参考用のみ)

細胞アッセイ	細胞株	WTK1 lymphoblasts
	濃度	1.0 μM
	反応時間	8 hours
	実験の流れ	XAV-939 is solubilized in DMSO at 55 °C to make a 10 mM stock solution which may be diluted later to a working concentration of 100 μM. WTK1 lymphoblasts treated with either DMSO or 1.0 μM of this compound for 8 hours are loaded into independent wells of a 4-20% gradient SDS-PAGE every 2 hours over the course of 6 hours. At each time point, DMSO and this chemical samples are loaded into wells immediately adjacent to the prior time point. The corresponding load times at 0, 2 and 4 hours results in total run times of 2, 4 and 6 hours respectively. The gel is analyzed via western blot for DNA-PKcs following completion of the final run time and is quantified after normalization to actin loading controls.
動物実験	動物モデル	Male Sprague-Dawley rats
	投薬量	3 mg/kg
	投与方法	i.p.

参考

https://pubmed.ncbi.nlm.nih.gov/21037379/
https://pubmed.ncbi.nlm.nih.gov/19759537/
https://pubmed.ncbi.nlm.nih.gov/33128175/

カスタマーフィードバック

: Data from [Data independently produced by Nat Commun, 2014, 5, 5455]

: Data from [Data independently produced by Dis Model Mech, 2014, 7(10), 1193-203]

: , , Cancer Lett, 2017, 400:194-202

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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。