IITZ-01

製品コードS8764 バッチS876401

印刷

化学情報

Synonyms

N/A

Storage
(From the date of receipt)

3 years -20°C powder

化学式

C₂₆H₂₃FN₈O

分子量

482.51

CAS No.

1807988-47-1

Solubility (25°C)*

体外

DMSO

100 mg/mL (207.24 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	2%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。	1.120mg/ml (2.32mM)	Taking the 1 mL working solution as an example, add 20 μL of 56 mg/ml clear DMSO stock solution to 980 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	IITZ-01 is a potent autophagy inhibitor, enhancing autophagosome accumulation but inhibiting autophagosomal degradation by impairing lysosomal function.
in vitro	Treatment with IITZ-01 results in the vacuolated appearance of cells due to its specific accumulation in lysosomes. It deacidifies lysosomes and inhibits maturation of lysosomal enzymes leading to lysosomal dysfunction. This compound enhances autophagosome accumulation but inhibits autophagosomal degradation by impairing lysosomal function, finally resulting in the inhibition of autophagy. It also abolishes mitochondrial membrane potential and triggered apoptosis through the mitochondria-mediated pathway. In in-vitro screening assays, this chemical shows negligible inhibition toward PI3K γ (IC50: 2.62 μM) and no significant inhibition at 10 μM against mTORC1. Immunoblotting experiment has revealed no significant decrease in p-AKT levels in breast cancer cells when treated with this agent. It can trigger apoptosis via disrupting MMP and modulating Bcl-2 and IAP family proteins^[1].
in vivo	This compound displays potent antitumor action in vivo through autophagy inhibition and apoptosis induction in MDA-MB-231 breast cancer xenograft model^[1].

プロトコル(参考用のみ)

細胞アッセイ	細胞株	MDA-MB-231 cells
	濃度	0.125-2 µM
	反応時間	24 h
	実験の流れ	MDA-MB-231 cells were treated with the designated concentrations (0.125-2 µM) of IITZ-01 and IITZ-02 for 24 h or 2 µM of this compound for specific time periods 3, 6, 12, 18, and 24 h. The protein expression levels of SQSTM1 were measured by western blotting experiment.
動物実験	動物モデル	MDA-MB-231/green fluorescent protein (GFP) orthotropic breast cancer xenografts (developed in CrTac:NCr-Foxnnu BALB/c female nude mice)
	投薬量	45 mg/kg every alternate day
	投与方法	i.p.

参考

https://pubmed.ncbi.nlm.nih.gov/30166591/

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 DR5 and Downregulation of Survivin by IITZ-01, Lysosomotropic Autophagy Inhibitor, Potentiates TRAIL-Mediated Apoptosis in Renal Cancer Cells via Ubiquitin-Proteasome Pathway [ Cancers (Basel), 2020, 12(9):E2363]	PubMed: 32825566

Upregulation of DR5 and Downregulation of Survivin by IITZ-01, Lysosomotropic Autophagy Inhibitor, Potentiates TRAIL-Mediated Apoptosis in Renal Cancer Cells via Ubiquitin-Proteasome Pathway [ Cancers (Basel), 2020, 12(9):E2363]

PubMed: 32825566

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。