APX-3330

製品コードS7445 バッチS744501

印刷

化学情報

Synonyms

E3330

Storage
(From the date of receipt)

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

化学式

C₂₁H₃₀O₆

分子量

378.46

CAS No.

136164-66-4

Solubility (25°C)*

体外

DMSO

100 mg/mL (264.22 mM)

Ethanol

75 mg/mL (198.17 mM)

Water

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。	5mg/ml (13.21mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 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。	0.71mg/ml (1.88mM)	Taking the 1 mL working solution as an example, add 50 μL of 14.2 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	APX-3330 (E3330) は強力で選択的なAPE1(Ref-1)阻害剤であり、NF-kappa B DNA結合活性を抑制しました。
in vitro	E3330 affects hemangioblast development in vitro via inhibition of Ape1 redox activity. E3330 inhibits the growth of human pancreatic cancer cell line PANC1, XPA1, MIAPACA, BxPC3, and PK9. E3330 also promotes exit of cell cycle in PANC1 cells, inhibits the DNA-Binding activity of HIF-1α and migration of pancreatic cancer cells. In JHH6 cells, E3330 prevents the functional activation of NF-κB via the alteration of APE1 subcellular trafficking and reduces IL-6 and IL-8 expression induced by TNF-α and FAs accumulation through blockage of the redox-mediated activation of NF-κB.
in vivo	In mice with endotoxin-mediated hepatitis, E3330 (300 mg/kg, p.o.) attenuates the elevation of plasma tumor necrosis factor activity and protectes mice from liver injury. In Rat model, E3330 (100 mg/kg, p.o.) also protectes rats from severe liver injury induced with endotoxin plus galactosamine.

プロトコル(参考用のみ)

細胞アッセイ	細胞株	PANC1 cells
	濃度	~30 μM
	反応時間	72 hours
	実験の流れ	PANC1 cells are placed in one well of a 12-well plate and treated with 5 to 30 μM E3330. After a 24, 48, and 72 h of culture, the cells are washed with PBS and stained with trypan blue, and cell viability is examined by counting the live cell numbers.
動物実験	動物モデル	Mice with endotoxin-mediated hepatitis
	投薬量	300 mg/kg
	投与方法	p.o.

参考

https://pubmed.ncbi.nlm.nih.gov/17053053/
https://pubmed.ncbi.nlm.nih.gov/18645011/
https://pubmed.ncbi.nlm.nih.gov/23967134/

https://pubmed.ncbi.nlm.nih.gov/1625194/
https://pubmed.ncbi.nlm.nih.gov/8423547/

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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：

Apex1 safeguards genomic stability to ensure a cytopathic T cell fate in autoimmune disease models [ J Clin Invest, 2024, e183671]	PubMed: 39739423
APE1 promotes non-homologous end joining by initiating DNA double-strand break formation and decreasing ubiquitination of artemis following oxidative genotoxic stress [ J Transl Med, 2023, 21(1):183]	PubMed: 36894994
Pharmacological inhibition of Ref-1 enhances the therapeutic sensitivity of papillary thyroid carcinoma to vemurafenib [ Cell Death Dis, 2022, 13(2):124]	PubMed: 35136031
Inhibiting the redox function of APE1 suppresses cervical cancer metastasis via disengagement of ZEB1 from E-cadherin in EMT [ J Exp Clin Cancer Res, 2021, 40(1):220]	PubMed: 34210327
Effect of Exosomal APE1 on Sensitivity of NSCLC A549 Cells to Cisplatin [ Cancer Research on Prevention and Treatment, 2020, (7): 492-497]	PubMed: None

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。