Erastin

製品コードS7242 バッチS724205

印刷

化学情報

Synonyms

N/A

Storage
(From the date of receipt)

3 years -20°C powder

化学式

C₃₀H₃₁ClN₄O₄

分子量

547.04

CAS No.

571203-78-6

Solubility (25°C)*

体外

DMSO (warmed with 50ºC water bath)

25 mg/mL (45.7 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。	1.000mg/ml (1.83mM)	Taking the 1 mL working solution as an example, add 50 μL of 20 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。	0.500mg/ml (0.91mM)	Taking the 1 mL working solution as an example, add 50 μL of 10 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	Erastin is a ferroptosis activator by acting on mitochondrial VDAC, exhibiting selectivity for tumor cells bearing oncogenic RAS. Solutions are unstable and should be fresh-prepared.
in vitro	Erastin is selectively lethal to oncogenic RAS-mutant cell lines, and triggers a unique iron-dependent form of non-apoptotic cell death called ferroptosis. ^[1] ^[2] This compound binds directly to VDAC2 and causes mitochondrial damage via ROS production in an NADH-dependent manner, which induces cell death in some tumor cells harbouring activating mutations in the RAS-RAF-MEK pathway. ^[3] In addition, this chemical, via inducing ROS-mediated CID (Caspase-independent cell death), strongly enhances the effect in WT EGFR cells. ^[4]
in vivo	Erastin is a ferroptosis activator by inhibiting voltage-dependent anion channels (VDAC2/VDAC3). This compound also inhibits cystine-glutamate antiporter (xCT).^[5]

製品説明

Erastin is a ferroptosis activator by acting on mitochondrial VDAC, exhibiting selectivity for tumor cells bearing oncogenic RAS. Solutions are unstable and should be fresh-prepared.

in vitro

Erastin is selectively lethal to oncogenic RAS-mutant cell lines, and triggers a unique iron-dependent form of non-apoptotic cell death called ferroptosis. ^[1] ^[2]

This compound binds directly to VDAC2 and causes mitochondrial damage via ROS production in an NADH-dependent manner, which induces cell death in some tumor cells harbouring activating mutations in the RAS-RAF-MEK pathway. ^[3]

In addition, this chemical, via inducing ROS-mediated CID (Caspase-independent cell death), strongly enhances the effect in WT EGFR cells. ^[4]

in vivo

Erastin is a ferroptosis activator by inhibiting voltage-dependent anion channels (VDAC2/VDAC3). This compound also inhibits cystine-glutamate antiporter (xCT).^[5]

プロトコル(参考用のみ)

細胞アッセイ	細胞株	BJ-TERT/LT/ST/RASV12 cells
	濃度	5 or 10 μg/mL
	反応時間	6-11 hours
	実験の流れ	BJ-TERT/LT/ST/RASV12 cells are seeded in 100 mm dishes and allowed to grow overnight. Cells are treated with erastin (5 or 10 μg/ml) for 6, 8, or 11 hr. A camptothecin-treated (0.4 μg/ml) control is maintained, treated at the time of seeding for 20 hours. After the treatment, cells are harvested with trypsin/EDTA and washed once with fresh medium containing serum and then twice with phosphate-buffered saline. Cells are resuspended in 1× binding buffer. 100 μL is incubated with 5 μL of Annexin V-FITC and propidium iodiode for 15 min in the dark at room temperature. Then 400 μl of the 1× binding buffer s added and the cells analyzed by flow cytometry. Data are acquired and analyzed using Cellquest software. Only viable cells that do not stain with propidium iodiode are analzyed for Annexin V-FITC staining using the FL1 channel.
動物実験	動物モデル	C57BL/6 mice
	投薬量	10 mg/kg
	投与方法	i.n.

参考

https://pubmed.ncbi.nlm.nih.gov/12676586/
https://pubmed.ncbi.nlm.nih.gov/22632970/
https://pubmed.ncbi.nlm.nih.gov/17568748/

https://pubmed.ncbi.nlm.nih.gov/23344263/
https://pubmed.ncbi.nlm.nih.gov/35197442/

+ 展开

カスタマーフィードバック

: , , Cancer Res, 2017, 77(8):2064-2077

: Data from [Data independently produced by , , Gastroenterology, 2017, 153(5):1429-1443]

: Data from [Data independently produced by , , Gastroenterology, 2018, 154(5):1480-1493]

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：

SIGLEC12 mediates plasma membrane rupture during necroptotic cell death [ Nature, 2025, 10.1038/s41586-025-09741-1]	PubMed: 41225007
The essential host genome for Cryptosporidium survival exposes metabolic dependencies that can be leveraged for treatment [ Cell, 2025, S0092-8674(25)00751-2]	PubMed: 40706591
Proteogenomic characterization of non-functional pancreatic neuroendocrine tumors unravels clinically relevant subgroups [ Cancer Cell, 2025, 43(4):776-796.e14]	PubMed: 40185092
Cytosolic cytochrome c represses ferroptosis [ Cell Metab, 2025, S1550-4131(25)00149-4]	PubMed: 40233758
Senescence-associated lysosomal dysfunction impairs cystine deprivation-induced lipid peroxidation and ferroptosis [ Nat Commun, 2025, 16(1):6617]	PubMed: 40731111
S100P is a ferroptosis suppressor to facilitate hepatocellular carcinoma development by rewiring lipid metabolism [ Nat Commun, 2025, 16(1):509]	PubMed: 39779666
Dysregulation of mitochondrial α-ketoglutarate dehydrogenase leads to elevated lipid peroxidation in CHCHD2-linked Parkinson's disease models [ Nat Commun, 2025, 16(1):1982]	PubMed: 40011434
Simvastatin overcomes the pPCK1-pLDHA-SPRINGlac axis-mediated ferroptosis and chemo-immunotherapy resistance in AKT-hyperactivated intrahepatic cholangiocarcinoma [ Cancer Commun (Lond), 2025, 10.1002/cac2.70036]	PubMed: 40443016
A transcriptional atlas of gut-innervating neurons reveals activation of interferon signaling and ferroptosis during intestinal inflammation [ Neuron, 2025, S0896-6273(25)00136-9]	PubMed: 40101721
HIF-independent oxygen sensing via KDM6A regulates ferroptosis [ Mol Cell, 2025, 85(15):2973-2987.e6]	PubMed: 40712585

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。