Erastin

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.

Erastin化学構造

CAS No. 571203-78-6

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Erastinと併用されることが多い化合物

RSL3


Erastin and RSL3 as ferroptosis inducers (FINs), sensitize cancer cells (H460/A549) to ionizing radiation (IR).


Lei G, et al. Cell Res. 2020;30(2):146-162.

FIN56


Erastin and FIN56, along with other ferroptosis inducers, restore trastuzumab sensitivity in rSKBR3-breast cancer cells.


Zou Y, et al. Nat Commun. 2022 May 13;13(1):2672.

Liproxstatin-1


Liproxstatin-1 protects against ferroptosis-inducing agents, such as Erastin and RSL3 in a dose-dependent manner.


Friedmann Angeli JP, et al. Nat Cell Biol. 2014;16(12):1180-1191.

Fer-1 (Ferrostatin-1)


Ferrostatin-1 promotes reversal of Erastin-induced ferroptosis in HT-22/HT-1080 dying cells.


Tang HM, et al. Biol Open. 2019 Jun 11;8(6):bio043182.

Z-VAD-FMK


Erastin and Z-VAD-FMK combination does not block erastin-induced cell death in HS578T/MDAMB231 cells.


Che C, et al. Cell Death Dis. 2022 Feb 14;13(2):150.

Erastin関連製品

Ferroptosis阻害剤の選択性比較

Cell Data

Cell Lines Assay Type Concentration Incubation Time 活性情報 PMID
human BJeLR cells Cytotoxic assay 10 μM 12 h Cytotoxicity against human BJeLR cells expressing RAS G12V mutant at 10 uM at 12 hrs by trypan blue staining 22832321
human BJ cells Function assay 9 μM Induction of cell death in human BJ cells expressing TERT, LT, ST and RAS G12V mutant genes cells at 9 uM. 17568748
human BJ cells Function assay 4.6 μM Increase in intracellular oxidative species in human BJ cells expressing TERT, LT, ST and RAS G12V mutant genes cells at 4.6 uM 17568748
human BJeH cells Function assay 6 h Induction of reactive oxygen species production in human BJeH cells expressing wild type RAS after 6 hrs by DCF-based flow cytometric analysis 22832321
human HeLa cells Function assay Induction of cell death in human HeLa cells, EC50=0.6 μM. 17568748
human BJ cells Function assay Induction of cell death in human BJ cells expressing TERT, LT, ST and RAS G12V mutant genes cells in presence of PD-98059 by trypan blue exclusion method, IC50=0.9 μM. 17568748
human HT1080 cells Function assay Induction of cell death in human HT1080 cells in presence of PD-98059 by trypan blue exclusion method, IC50=1 μM. 17568748
human SVR cells Function assay Induction of cell death in human SVR cells, EC50=2.5 μM. 17568748
human SKUT cells Function assay Induction of cell death in human SKUT cells, EC50=4 μM. 17568748
human MES-SA cells Function assay Induction of cell death in human MES-SA cells, EC50=3 μM. 17568748
human Calu1 cells Function assay Inhibition of human Calu1 cells expressing KRAS with activating mutations by trypan blue exclusion assay, IC50=4 μM. 17568748
human LNCaP cells Function assay Induction of cell death in human LNCaP cells, EC50=6 μM. 17568748
human U2OS cells Function assay Induction of cell death in human U2OS cells, EC50=6 μM. 17568748
human TC32 cells Function assay Induction of cell death in human TC32 cells 17568748
human U937 cells Function assay Induction of cell death in human U937 cells, EC50=10 μM. 17568748
human SK-N-MC cells Function assay Induction of cell death in human SK-N-MC cells, EC50=10 μM. 17568748
human TC71 cells Function assay Induction of cell death in human TC71 cells, EC50=10 μM. 17568748
human EWS502 cells Function assay Induction of cell death in human EWS502 cells, EC50=10 μM. 17568748
human BJ cells Function assay Induction of cell death in TERT expressing human BJ cells, EC50=10 μM. 17568748
human Hs51.T cells Function assay Induction of cell death in human Hs51.T cells, EC50=12 μM. 17568748
human Hs925.T cells Function assay Induction of cell death in human Hs925.T cells, EC50=17 μM. 17568748
human HOS cells Function assay Induction of cell death in human HOS cells , EC50=17 μM. 17568748
human MX2 cells Function assay Induction of cell death in human MX2 cells, EC50=18 μM. 17568748
human A673 cells Function assay Induction of cell death in human A673 cells, EC50=30 μM. 17568748
human BJ cells Function assay Induction of cell death in human BJ cells expressing TERT, LT, ST and RAS G12V mutant genes in presence of U0126 by trypan blue exclusion method, IC50=31.2 μM. 17568748
human CCF-STTG1 cells Function assay Inhibition of Xct in human CCF-STTG1 cells assessed as glutamate release after 2 hrs by fluorometry, IC50=0.2 μM. 26231156
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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.
Targets
Ferroptosis [1]
In Vitro
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]

細胞実験 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.

実験結果図 Methods Biomarkers 結果図 PMID
Western blot GPX4 / cleaved-PARP / cleaved-caspase3 / LC3 / p62 / LDH / HMGB1 TfR1 / p-JNK / JNK / p-P38 HSPA5 / p-EIF2AK3 GRP78 27308510
Growth inhibition assay Cell survival 29348676
Immunofluorescence HMGB1 31105999
In Vivo
In Vivo

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

動物実験 動物モデル C57BL/6 mice
投与量 10 mg/kg
投与経路 i.n.

化学情報

分子量 547.04 化学式

C30H31ClN4O4

CAS No. 571203-78-6 SDF Download Erastin SDFをダウンロードする
Smiles CCOC1=CC=CC=C1N2C(=O)C3=CC=CC=C3N=C2C(C)N4CCN(CC4)C(=O)COC5=CC=C(C=C5)Cl
保管 3 years -20°C powder 溶液状態は不安定なので使用直前に調整してください。少量づつ分包して保管し、都度使い切る事が推奨されます。

In vitro
Batch:

DMSO : 25 mg/mL ( (45.7 mM); Warmed with 50℃ water bath; 吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Water : Insoluble

Ethanol : Insoluble

モル濃度計算器

in vivo
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機

実験計算

モル濃度計算器

質量 濃度 体積 分子量

投与溶液組成計算機(クリア溶液)

ステップ1:実験データを入力してください。(実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します)

mg/kg g μL

ステップ2:投与溶媒の組成を入力してください。(ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください)

% DMSO % % Tween 80 % ddH2O
%DMSO %

計算結果:

投与溶媒濃度: mg/ml;

DMSOストック溶液調製方法: mg 試薬を μL DMSOに溶解する(濃度 mg/mL, 注:濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法:Take μL DMSOストック溶液に μL PEG300,を加え、完全溶解後μL Tween 80,を加えて完全溶解させた後 μL ddH2O,を加え完全に溶解させます。

投与溶媒調製方法:μL DMSOストック溶液に μL Corn oil,を加え、完全溶解。

注意:1.ストック溶液に沈殿、混濁などがないことをご確認ください;
2.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

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