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Erastin Sale

Catalog No.GC16630

Erastin is a cell-permeable ferroptosis activatior and antitumor agent.

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Erastin Chemical Structure

Cas No.: 571203-78-6

Size Price Stock Qty
1mg
$35.00
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5mg
$77.00
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10mg
$115.00
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50mg
$300.00
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Sample solution is provided at 25 µL, 10mM.

Product has been cited by 15 publications

Product Documents

Quality Control & SDS

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Protocol

Cell experiment [1]:

Cell lines

143B/BJeHLT/BJeLR/Calu-1/HT-1080

Preparation Method

Soluble in DMSO to 20 mM.

Reaction Conditions

10 μM, 72 h

Applications

Erastin inhibited cystine uptake via system xc and triggered ferroptosis in a variety of cellular contexts.(HT-1080: erastin IC50 = 0.20 µM; Calu-1: erastin IC50 = 0.14 µM)

Animal experiment [2]:

Animal models

BALB/c nude mice (colorectal cancer)

Preparation Method

Soluble in DMSO to 20 mM

Dosage form

10 mg/kg, intravenous injection

Applications

Erastin inhibited ALDH1 activity, and reduced sphere size and number in colorectal cancer cells.

References:

[1]. Dixon SJ, et al. Pharmacological inhibition of cystine-glutamate exchange induces endoplasmic reticulum stress and ferroptosis. Elife. 2014 May 20;3:e02523.

[2]. Xu X, et al. Targeting SLC7A11 specifically suppresses the progression of colorectal cancer stem cells via inducing ferroptosis. Eur J Pharm Sci. 2020 Sep 1;152:105450.

Background

Erastin is a cell-permeable ferroptosis activatior and an antitumor agent that is selective for cell expressing oncogene RAS.

Erastin induces ferroptosis through directly binding to VDAC2/3 to alter the permeability of the outer mitochondrial membrane, which decreases the rate of NADH oxidation. Besides exerting targeted effects, erastin also enhances chemotherapy, targeted therapy, and immunotherapy in certain cancer cells, suggesting a potential role of erastin in cancer cell treatment.[3]

Erastin and its analogs specifically inhibited cystine uptake via system xc, and triggered ferroptosis in a variety of cellular contexts and act much more potently than SAS. Moreover, Erastin was ∼2500 times more potent than SAS as an inhibitor of system xc function in both HT-1080 and Calu-1 cells (HT-1080: erastin IC50 = 0.20 µM, SAS IC50 = 450 µM; Calu-1: erastin IC50 = 0.14 µM, SAS IC50 = 460 µM).[1]

Erastin, an inhibitor of SLC7A11, was found to hold a remarkably stronger cytotoxic effect on colorectal CSCs via in vitro and in vivo experiments. Besides, Erastin attenuated the chemoresistance of colorectal CSCs (colorectal cancer stem cells). For in vivo experiment, Erastin (10 mg/kg) was intravenously injected into mice with colorectal cancer every two days. It was found that Erastin inhibited ALDH1 activity, and reduced sphere size and number in colorectal cancer cells. [2]

References:
[1]. Dixon SJ, et al. Pharmacological inhibition of cystine-glutamate exchange induces endoplasmic reticulum stress and ferroptosis. Elife. 2014 May 20;3:e02523.
[2]. Xu X, et al. Targeting SLC7A11 specifically suppresses the progression of colorectal cancer stem cells via inducing ferroptosis. Eur J Pharm Sci. 2020 Sep 1;152:105450.
[3]. Yang Y, et al. Nedd4 ubiquitylates VDAC2/3 to suppress erastin-induced ferroptosis in melanoma. Nat Commun. 2020 Jan 23;11(1):433.

Chemical Properties

Cas No. 571203-78-6 SDF
Chemical Name 2-[1-[4-[2-(4-chlorophenoxy)acetyl]piperazin-1-yl]ethyl]-3-(2-ethoxyphenyl)quinazolin-4-one
Canonical SMILES O=C1N(C2=CC=CC=C2OCC)C(C(N3CCN(C(COC4=CC=C(Cl)C=C4)=O)CC3)C)=NC5=C1C=CC=C5
Formula C30H31ClN4O4 M.Wt 547.04
Solubility ≥ 10.92mg/mL in DMSO with gentle warming ,This product is unstable in solution and it is recommended to prepare and use it immediately. Storage Store at -20° C
General tips This product is unstable in nature and needs to be prepared and used immediately! It is recommended that you purchase small-sized packages, or repack small-sized ones after receiving the goods.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 1.828 mL 9.1401 mL 18.2802 mL
5 mM 0.3656 mL 1.828 mL 3.656 mL
10 mM 0.1828 mL 0.914 mL 1.828 mL
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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.
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3. All of the above co-solvents are available for purchase on the GlpBio website.

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    Erastin- GlpBio

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