Adavivint (SM04690)

製品コードS8761 バッチS876101

印刷

化学情報

Synonyms

Lorecivivint

Storage
(From the date of receipt)

3 years -20°C powder

化学式

C₂₉H₂₄FN₇O

分子量

505.55

CAS No.

1467093-03-3

Solubility (25°C)*

体外

DMSO

30 mg/mL (59.34 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 40%PEG300 2 5%Tween80 3 50%ddH2O 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。	0.750mg/ml (1.48mM)	Taking the 1 mL working solution as an example, add 50 μL of 15 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% 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。	0.180mg/ml (0.36mM)	Taking the 1 mL working solution as an example, add 50 μL of 3.6 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	Adavivint (SM04690, Lorecivivint) は、TCF/LEFレポーターを阻害するEC50が19.5 nMである、canonical Wntシグナル伝達の強力で特異的な阻害剤です。これは、複数の細胞アッセイにおいて、他の既知のWnt阻害剤よりも約150〜500倍強力です。
in vitro	Adavivint (SM04690) induces a dose-dependent decrease in the expression of Wnt pathway genes (ASCL1, LEF1, TCF7L2, TCF7, C-262 MYC and AXIN2) in bone-marrow-derived hMSCs (CD29+, CD44+ CD166+ CD105+ CD45-). This compound also inhibits the expression of AXIN2, TCF7 and LEF1 in hMSCs and AXIN2 and LGR5 in IEC6 (intestinal stem cells sensitive to Wnt activation) when the Wnt pathway is selectively activated using either Wnt3a or a GSK3β inhibitor, CHIR-99021. It has minimal effects on the non-canonical Wnt pathway and the BMP pathway, and protects chondrocytes from catabolic breakdown in vitro.
in vivo	In a rat model of knee osteoarthritis, intra-articular injection of Adavivint (SM04690) promotes cartilage growth and improves joint health. It decreases cartilage breakdown in vivo.

プロトコル(参考用のみ)

細胞アッセイ	細胞株	SW480 cells and hMSCs
	濃度	10, 30 and 100 nM
	反応時間	48 h
	実験の流れ	Adavivint (SM04690) is described in the following text: --
動物実験	動物モデル	Sprague-Dawley (SD) rats (12 weeks old, male)
	投薬量	0.3μg in 50μl
	投与方法	intra-articular injection

参考

https://pubmed.ncbi.nlm.nih.gov/28888902/

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：

Methylation-modulated PFTK1 regulates gefitinib resistance via Wnt/β-catenin signaling in EGFR mutant non-small-cell lung cancer cells [ Commun Biol, 2024, 7(1):1649]	PubMed: 39702755
Pharmacological inhibition of CLK2 activates YAP by promoting alternative splicing of AMOTL2 [ Elife, 2023, 12RP88508]	PubMed: 38126343
Canonical Wnt Pathway Is Involved in Chemoresistance and Cell Cycle Arrest Induction in Colon Cancer Cell Line Spheroids [ Int J Mol Sci, 2023, 24(6)5252]	PubMed: 36982333
"Pharmacological inhibition of CLK2 activates YAP by promoting alternative splicing of AMOTL2" [ bioRxiv, 2023, 2023.04.19.537449]	PubMed: 37131806
β-catenin regulates HIV latency and modulates HIV reactivation [ PLoS Pathog, 2022, 18(3):e1010354]	PubMed: 35255110
Glycyrrhizic acid alters the hyperoxidative stress-induced differentiation commitment of MSCs by activating the Wnt/β-catenin pathway to prevent SONFH [ Food Funct, 2022, 10.1039/d2fo02337g]	PubMed: 36541285
Engineering osteoarthritic cartilage model through differentiating senescent human mesenchymal stem cells for testing disease-modifying drugs [ Sci China Life Sci, 2021, 10.1007/s11427-021-1933-7]	PubMed: 34109475
Inhibiting Wnt/beta-catenin in CTNNB1-mutated endometrial cancer [ Mol Carcinog, 2021, 10.1002/mc.23308]	PubMed: 34038589

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。