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Purity: ≥98%
Erastin is a cell-permeable small molecule and potent ferroptosis activator by acting on mitochondrial VDAC with potential antineoplastic activity. It exhibits selectivity for tumor cells bearing oncogenic RAS and shows high in vivo antitumor efficacy in mice with HT-29 xenograft. Erastin is an antitumor agent selective for tumor cells bearing oncogenic RAS (i.e. HRAS, KRAS). Ferroptosis is a unique iron-dependent form of nonapoptotic cell death. It is triggered by oncogenic RAS-selective lethal small molecule erastin. Acitvation of ferroptosis lead to nonapoptotic destruction of cancer cells.
ln Vitro |
Ferroptosis in ectopic endometrial stromal cells (EESC) is triggered by erematin (10 μM; 24 hours), and at 9 hours, total ROS levels rise [1]. In EESC cells, erythrin can reduce the length of mitochondria and raise their membrane density [1]. Iron-related proteins, including FPN (iron export protein), have lower levels of mRNA expression in EESCs when treated with erythrin (10 μM) for nine hours. On the other hand, overexpression of FPN can considerably prevent Erastin-induced ferroptosis of EESCs [1]. In HT-29 colorectal cancer cells, erematin (10 μM; 24 hours) causes the opening of the mitochondrial permeability transition pore (mPTP) [2]. The proliferation of HT-29 colorectal cancer cells is greatly inhibited by eratin (30 μM; 72 hours) [2]. The genes that control iron metabolism or mitochondrial fatty acid metabolism are involved in the biological mechanism by which erythropoidin triggers ferroptosis. comprises tetrapeptide repeat domain 35, citrate synthase, ATP synthase F0 complex subunit C3, ribosomal protein L8, iron response element binding protein 2 (IREB2), and acyl-CoA synthetase family member 2 (ACSF2)[3].
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ln Vivo |
Ferroptosis-induced animal models can be created with erastibin. In a mouse model of endometriosis, Erastin (40 mg/kg; i.p.; every 3 days for 2 weeks) inhibits endometriotic implantation, indicating that Erastin promotes regression of ectopic lesions by inducing ferroptosis [1]. In SCID mice, eratin (10 mg/kg, 30 mg/kg; intraperitoneally; once daily for 4 weeks) suppresses the growth of HT-29 xenografts, with 30 mg/kg showing the greatest activity [2].
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Cell Assay |
Cell Viability Assay[1]
Cell Types: Normal endometrial stromal cells (NESCs) and endometrial stromal cells (EESCs) Tested Concentrations: 0, 0.5, 0.8, 1, 1.5, 2, 2.5, 5, 10 μM Incubation Duration: 24 hrs (hours) Experimental Results: Induced cell detachment and overt death in EESCs, but not NESCs. Apoptosis Analysis[1] Cell Types: EESCs infected with adenovirus expressing FPN cDNA (co-incubation for 24 hr) Tested Concentrations: 0, 0.5, 1.5, 2.5, 5 and 2.5 μM Incubation Duration: 24 hrs (hours) Experimental Results: Induced ferroptosis by decreasing the levels of total ROS and lipid ROS. And reversed by the overexpression of FPN in adenovirus-infected cells. |
Animal Protocol |
Animal/Disease Models: Mouse model of endometriosis[1]
Doses: 40 mg/kg Route of Administration: intraperitoneal (ip)injection; once every 3 days for 2 weeks Experimental Results: demonstrated little impact on body weight of mice and hair of mice displayed neat and glossy. decreased the volume of ectopic lesions. |
References |
[1]. Li Y, et al. Erastin induces ferroptosis via ferroportin-mediated iron accumulation in endometriosis. Hum Reprod. 2021 Mar 18;36(4):951-964.
[2]. Huo H, et al. Erastin Disrupts Mitochondrial Permeability Transition Pore (mPTP) and Induces Apoptotic Death of Colorectal Cancer Cells. PLoS One. 2016 May 12;11(5):e0154605. [3]. Xie Y, et al. Ferroptosis: process and function. Cell Death Differ. 2016 Mar;23(3):369-79. |
Molecular Formula |
C30H31CLN4O4
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Molecular Weight |
547.04
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CAS # |
571203-78-6
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SMILES |
O=C1N(C2=CC=CC=C2OCC)C(C(N3CCN(C(COC4=CC=C(Cl)C=C4)=O)CC3)C)=NC5=C1C=CC=C5
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Synonyms |
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
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Solubility (In Vivo) |
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Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 1.8280 mL | 9.1401 mL | 18.2802 mL | |
5 mM | 0.3656 mL | 1.8280 mL | 3.6560 mL | |
10 mM | 0.1828 mL | 0.9140 mL | 1.8280 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.