Erastin |
Catalog No.GC16630 |
Erastin is a cell-permeable ferroptosis activatior and antitumor agent.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 571203-78-6
Sample solution is provided at 25 µL, 10mM.
- Biomed Pharmacother (2023): 11479.5PMID:37146415
- Biochem Pharmacol (2023): 115592.PMID:37196680
- Cell Biol Toxicol (2023): 1-16.PMID:37266730
- Front Oncol 12 (2022): 930654.PMID:36033479
- J Sci Food Agric (2023).PMID:37850313
- Free Radical Bio Med 209 (2023): 135-150.PMID:37805047
- Cell Signal 114 (2024):111006.PMID:38086436
- Ecotox Environ Safe 271 (2024):115994.PMID:38262094
- J Sci Food Agr (2024).PMID:37850313
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Related Biological Data
(A) ALDH1 activity was measured in HT-29 cells after being treated with Erastin or not for 48 h. (B and C) Sphere size and number were evaluated in HT-29 cells after being treated with or without Erastin for 10 days.
Cisplatin (Cat # GC11908) and Erastin (Cat #GC16630) were purchased from GlpBio(Montclair, CA, USA). HT-29 cells were initially cultured with cisplatin (1 μM) and monoclonal cells were selected and expanded in medium containing 1 nM cisplatin for at least 6 months. Cells were cultured in RPMI 1640 medium containing 10% FBS in 37 °C and 5% CO2.
Eur J Pharm Sci (2020): 105450. -
Related Biological Data
Effect of propofol on erastin-induced H9C2 cell ferroptosis. (A). Cell viability of H9C2 cells treated with erastin (0–20 μM). (B): Effect of propofol on erastin-induced cell death.
H9C2 cells were treated with no reagents (C), erastin (5 μM, GC16630, California, GLPBIO, United States) for 24 h (E), and propofol (50 μM) for 1 h before erastin (E + P).
Front Pharmacol 13 (2022): 841410-841410
Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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. |
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.
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. |
Prepare stock solution | |||
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 |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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.)
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.
3. All of the above co-solvents are available for purchase on the GlpBio website.
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