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Erastin

Name: Erastin
Brand: Selleck Chemicals
SKU: S7242
Rating: 5 (387 reviews)

Catalog No.S7242 Purity: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.

Erastin Chemical Structure

CAS No. 571203-78-6

Purity & Quality Control

Batch: Purity: 99.89%

99.89

Products often used together with Erastin

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 Related Products

Related Products	Fer-1 (Ferrostatin-1) RSL3 Liproxstatin-1 FIN56 IKE(Imidazole ketone erastin) UAMC-3203 iFSP1 SRS16-86 SRS11-92	Click to Expand
Related Compound Libraries	Metabolism Compound Library Anti-cancer Metabolism Compound Library Glutamine Metabolism Compound Library Carbohydrate Metabolism Compound Library Lipid Metabolism Compound Library	Click to Expand

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	Activity Description	PMID
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 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	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 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			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 A673 cells	Function assay			Induction of cell death in human A673 cells, EC50=30 μM.	17568748
human MX2 cells	Function assay			Induction of cell death in human MX2 cells, EC50=18 μM.	17568748
human HOS cells	Function assay			Induction of cell death in human HOS cells , EC50=17 μM.	17568748
human Hs925.T cells	Function assay			Induction of cell death in human Hs925.T cells, EC50=17 μM.	17568748
human Hs51.T cells	Function assay			Induction of cell death in human Hs51.T cells, EC50=12 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 TC71 cells	Function assay			Induction of cell death in human TC71 cells, EC50=10 μM.	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 TC32 cells	Function assay			Induction of cell death in human TC32 cells	17568748
human U2OS cells	Function assay			Induction of cell death in human U2OS cells, EC50=6 μM.	17568748
human LNCaP cells	Function assay			Induction of cell death in human LNCaP cells, EC50=6 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 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 SVR cells	Function assay			Induction of cell death in human SVR cells, EC50=2.5 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 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 HeLa cells	Function assay			Induction of cell death in human HeLa cells, EC50=0.6 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
Click to View More Cell Line Experimental Data

Biological Activity

Description

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]
Cell Research	Cell lines	BJ-TERT/LT/ST/RASV12 cells
	Concentrations	5 or 10 μg/mL
	Incubation Time	6-11 hours
	Method	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.
Experimental Result Images	Methods	Biomarkers	Images	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]
Animal Research	Animal Models	C57BL/6 mice
	Dosages	10 mg/kg
	Administration	i.n.

References

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Chemical Information & Solubility

Molecular Weight	547.04	Formula	C₃₀H₃₁ClN₄O₄
CAS No.	571203-78-6	SDF	Download Erastin SDF
Smiles	CCOC1=CC=CC=C1N2C(=O)C3=CC=CC=C3N=C2C(C)N4CCN(CC4)C(=O)COC5=CC=C(C=C5)Cl
Storage (From the date of receipt)	3 years -20°C powder	Solutions are unstable. Prepare fresh or purchase small, pre-packaged sizes. Repackage upon receipt.

In vitro
Batch:

DMSO : 25 mg/mL ( (45.7 mM) Warmed with 50°C water bath; Ultrasonicated; Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molecular Weight Calculator

In vivo Batch: Add solvents to the product individually and in order.					In vivo Formulation Calculator
	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.	In vivo Formulation Calculator
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.

Preparing Stock Solutions

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
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Dilution Calculator Molecular Weight Calculator

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3
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