iCRT14

製品コードS8704 バッチS870401

印刷

化学情報

Synonyms

N/A

Storage
(From the date of receipt)

3 years -20°C powder

化学式

C₂₁H₁₇N₃O₂S

分子量

375.44

CAS No.

677331-12-3

Solubility (25°C)*

体外

DMSO

37 mg/mL (98.55 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。	2.000mg/ml (5.33mM)	Taking the 1 mL working solution as an example, add 50 μL of 40 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。	2.000mg/ml (5.33mM)	Taking the 1 mL working solution as an example, add 50 μL of 40 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	iCRT14 is a β-catenin/Tcf inhibitor with a Ki value of 54 ± 5.2 μM in homogeneous fluorescence polarization (FP) assay.
in vitro	iCRT14 suppresses the transcriptional activity of canonical Wnt signaling, downregulates Wnt/β-catenin-induced target genes, and inhibits the growth of colorectal cancer cells in vitro^[1]. This compound shows a modest reduction in the amount of Dvl but has no effect on Dvl phosphorylation itself. It inhibits the Wnt responsive STF16-luc reporter in mammalian HEK293 cells with an IC50 of 40.3 nM. This chemical can also interfere with TCF binding to DNA in addition to its ability to influence TCF-β-catenin interaction^[2].
in vivo	Administration of iCRT14 to the HCT116 and HT29 xenograft models reveals a marked decrease in CycD1, coincided with reduced proliferation of the tumors. Furthermore, these effects are correlated with a marked reduction (∼50%) in the initial growth rate of tumors within the first 3 wk (∼day 19) of this compound administration. After day 19, however, the rate of tumor growth is comparable with that of DMSO-treated control. Throughout the course of the study, the mice does not display any signs of systemic toxicity or weight loss that would indicate off-target or nonspecific effects. This compound may be metabolized rapidly in vivo, thus reducing its bioavailability^[2].

プロトコル(参考用のみ)

細胞アッセイ	細胞株	Rat2 cells
	濃度	25 and 50 μM
	反応時間	2 h
	実験の流れ	Rat2 cells are pretreated with iCRT14 at the indicated doses and stimulated for 2 h with Wnt3a or Wnt5a. Cell lysate is harvested for western analysis of Dvl2 phosphorylation.
動物実験	動物モデル	HCT116 and HT29 xenograft models (implanted tumor cells in athymic nude mice)
	投薬量	50 mg/kg
	投与方法	i.p.

参考

https://pubmed.ncbi.nlm.nih.gov/25985283/
https://pubmed.ncbi.nlm.nih.gov/21393571/

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：

Upregulation of β-catenin signaling represents a single common pathway leading to the various phenotypes of spinal degeneration and pain [ Bone Res, 2023, 11(1):18]	PubMed: 37059724
Regulation of the WNT-CTNNB1 signaling pathway by severe fever with thrombocytopenia syndrome virus in a cap-snatching manner [ mBio, 2023, e0168823.]	PubMed: 37882780
β-catenin regulates HIV latency and modulates HIV reactivation [ PLoS Pathog, 2022, 18(3):e1010354]	PubMed: 35255110
Cytoplasmic SHMT2 drives the progression and metastasis of colorectal cancer by inhibiting β-catenin degradation [ Theranostics, 2021, 11(6):2966-2986]	PubMed: 33456583

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。