Erastin

Catalog No.S7242 Batch:S724204

Technical Data

Formula

C₃₀H₃₁ClN₄O₄

Molecular Weight

547.04

CAS No.

571203-78-6

Solubility (25°C)*

In vitro

DMSO (warmed with 50ºC water bath)

25 mg/mL (45.7 mM)

Water

Insoluble

Ethanol

Insoluble

In vivo (Add solvents to the product individually and in order)

Clear solution

10%DMSO 1 40%PEG300 2 5%Tween80 3 45%ddH2O

1.67mg/ml

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.

* <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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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

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]

In vivo

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

Protocol (from reference)

Cell Assay:^{^[1]}	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.
Animal Study:^{^[5]}	Animal Models C57BL/6 mice Dosages 10 mg/kg Administration i.n.

Cell Assay:^{^[1]}

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.

Animal Study:^{^[5]}

Animal Models
C57BL/6 mice
Dosages
10 mg/kg
Administration
i.n.

References

+ Expand

Customer Product Validation

: , , 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]

: Data from [Data independently produced by , , Hepatology, 2016, 64(2):488-500.]

Selleck's Erastin has been cited by 418 publications

Sensing steroid hormone 17α-hydroxypregnenolone by GPR56 enables protection from ferroptosis-induced liver injury [ Cell Metab, 2024, S1550-4131(24)00371-1]	PubMed: 39389061
Pro-ferroptotic signaling promotes arterial aging via vascular smooth muscle cell senescence [ Nat Commun, 2024, 15(1):1429]	PubMed: 38365899
SLC13A3 is a major effector downstream of activated β-catenin in liver cancer pathogenesis [ Nat Commun, 2024, 15(1):7522]	PubMed: 39215042
IRE1α determines ferroptosis sensitivity through regulation of glutathione synthesis [ Nat Commun, 2024, 15(1):4114]	PubMed: 38750057
A novel MYC-ZNF706-SLC7A11 regulatory circuit contributes to cancer progression and redox balance in human hepatocellular carcinoma [ Cell Death Differ, 2024, 10.1038/s41418-024-01324-3]	PubMed: 38862581
PRMT6-mediated ADMA promotes p62 phase separation to form a negative feedback loop in ferroptosis [ Theranostics, 2024, 14(10):4090-4106]	PubMed: 38994016
HiHo-AID2: boosting homozygous knock-in efficiency enables robust generation of human auxin-inducible degron cells [ Genome Biol, 2024, 25(1):58]	PubMed: 38409044
LACTB suppresses liver cancer progression through regulation of ferroptosis [ Redox Biol, 2024, 75:103270]	PubMed: 39047638
Cold atmospheric plasma enhances SLC7A11-mediated ferroptosis in non-small cell lung cancer by regulating PCAF mediated HOXB9 acetylation [ Redox Biol, 2024, 75:103299]	PubMed: 39127016
Excessive SOX8 reprograms energy and iron metabolism to prime hepatocellular carcinoma for ferroptosis [ Redox Biol, 2024, 69:103002]	PubMed: 38142583

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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