Erastin

製品コード：S7242 純度：99.89%

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.

CAS No. 571203-78-6

サイズ	価格(税別)	在庫状況
1mg	JPY 22000	国内在庫あり
2mg	JPY 29500	国内在庫あり
1mg*5	JPY 41500	国内在庫なし(納期7~10日)
50mg	JPY 115500	国内在庫あり
200mg	JPY 190500	国内在庫あり
1g	JPY 295500	国内在庫なし(納期7~10日)

代表番号: 045-509-1970\|電子メール：[email protected] よく尋ねられる質問

文献中Selleckの製品使用例（400）

製品安全説明書

現在のバッチを見る：純度： 99.89%

99.89

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.

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.

Celastrol

Combined treatment induce cell death at nontoxic concentrations

Liu M,et al. Mol Oncol. 2021 Aug;15(8):2084-2105.

Erastin関連製品

関連製品	Fer-1 (Ferrostatin-1) RSL3 Liproxstatin-1 FIN56 IKE(Imidazole ketone erastin) UAMC-3203 iFSP1 SRS16-86 SRS11-92	もっと見る
関連化合物ライブラリー	Metabolism Compound Library Anti-cancer Metabolism Compound Library Glutamine Metabolism Compound Library Carbohydrate Metabolism Compound Library Lipid Metabolism Compound Library	もっと見る

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 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.

参考
[1] Dolma S, et al. Cancer Cell. 2003, 3(3), 285-296. [2] Dixon SJ, et al. Cell. 2012, 149(5), 1060-1072. [3] Yagoda N, et al. Nature. 2007 , 447(7146), 864-868. [4] Yamaguchi H, et al. Clin Cancer Res. 2013, 19(4), 845-854. [5] Tuo QZ, et al. Signal Transduct Target Ther. 2022 Feb 23;7(1):59. + 展開

参考

+ 展開

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; Ultrasonicated; 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
	Clear solution	10%DMSO 1 40%PEG300 2 5%Tween80 3 45%ddH2O	1.67mg/ml (3.05mM)	Taking the 1 mL working solution as an example, add 100 μL of 16.67 mg/ml clear 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 450 μL of ddH2O to make it clear. Volume up to 1 mL. The mixed solution should be used immediately for optimal results.	投与溶液組成計算機
Clear solution	10%DMSO 1 90%Corn oil	2.5mg/ml (4.57mM)	Taking the 1 mL working solution as an example, add 100 μL of 25 mg/ml clear DMSO stock solution to 900 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O	1.0mg/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	0.5mg/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.
Clear solution	10%DMSO 1 40%PEG300 2 5%Tween80 3 45%ddH2O	0.8mg/ml (1.46mM)	Taking the 1 mL working solution as an example, add 100 μL of 8 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 make it clear; then continue to add 450 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

実験計算

モル濃度計算器

質量	濃度	体積	分子量
=	×	×

希釈計算器分子量計算器

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）

投与量 mg/kg 動物平均体重 g 投与体積（動物毎）μL 動物数匹

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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