Erastin

製品コードS7242 バッチS724205

印刷

化学情報

Chemical Structure 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) 15 mg/mL (27.42 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）
Clear solution
5% DMSO 95% Corn oil
0.5mg/ml 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. 
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
1.0mg/ml 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. 
* <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]

Erastin 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, erastin, via inducing ROS-mediated CID (Caspase-independent cell death), strongly enhances the effect of cisplatin in WT EGFR cells. [4]
in vivo

Erastin is a ferroptosis activator by inhibiting voltage-dependent anion channels (VDAC2/VDAC3). It 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.

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：

Pro-ferroptotic signaling promotes arterial aging via vascular smooth muscle cell senescence [ Nat Commun, 2024, 15(1):1429] PubMed: 38365899
HiHo-AID2: boosting homozygous knock-in efficiency enables robust generation of human auxin-inducible degron cells [ Genome Biol, 2024, 25(1):58] PubMed: 38409044
Excessive SOX8 reprograms energy and iron metabolism to prime hepatocellular carcinoma for ferroptosis [ Redox Biol, 2024, 69:103002] PubMed: 38142583
Meningioma achieves malignancy and erastin-induced ferroptosis resistance through FOXM1-AURKA-NRF2 axis [ Redox Biol, 2024, 72:103137] PubMed: 38642502
SPTBN2 suppresses ferroptosis in NSCLC cells by facilitating SLC7A11 membrane trafficking and localization [ Redox Biol, 2024, 70:103039] PubMed: 38241838
Differentiation of intestinal stem cells toward goblet cells under systemic iron overload stress are associated with inhibition of Notch signaling pathway and ferroptosis [ Redox Biol, 2024, 72:103160] PubMed: 38631120
Hspb1 protects against severe acute pancreatitis by attenuating apoptosis and ferroptosis via interacting with Anxa2 to restore the antioxidative activity of Prdx1 [ Int J Biol Sci, 2024, 20(5):1707-1728] PubMed: 38481805
Caspase-2 protects against ferroptotic cell death [ Cell Death Dis, 2024, 15(3):182] PubMed: 38429264
Neutrophil extracellular traps mediate cardiomyocyte ferroptosis via the Hippo-Yap pathway to exacerbate doxorubicin-induced cardiotoxicity [ Cell Mol Life Sci, 2024, 81(1):122] PubMed: 38456997
Salidroside pretreatment alleviates ferroptosis induced by myocardial ischemia/reperfusion through mitochondrial superoxide-dependent AMPKα2 activation [ Phytomedicine, 2024, 155365] 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。

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