- Erastin
-
-
2026-07-27
- CAS:571203-78-6
- Purity: 99.69%
- Supply Ability: 10g
|
| | Erastin Basic information |
| Product Name: | Erastin | | Synonyms: | 2-[1-[4-[2-(4-Chlorophenoxy)acetyl]-1-piperazinyl]ethyl]-3-(2-ethoxyphenyl)-4(3H)-Quinazolinone;4(3H)-Quinazolinone, 2-[1-[4-[2-(4-chlorophenoxy)acetyl]-1-piperazinyl]ethyl]-3-(2-ethoxyphenyl)-;2-[1-[4-[2-(4-Chlorophenoxy)acetyl]-1-piperazinyl]ethyl]-3-(2-ethoxyphenyl)-4(3H)-quinazolinone Erastin;Erastin;CS-1430;Erastin - CAS 571203-78-6 - Calbiochem;2-(1-(4-(2-(4-Chlorophenoxy)acetyl)piperazin-1-yl)ethyl)-3-(2-ethoxyphenyl)quinazolin-4(3H)-on;2-(1-(4-(2-(4-Chlorophenoxy)acetyl)piperazin-1-yl)ethyl)-3-(2-ethoxyphenyl)quinazolin-4(3H)-one | | CAS: | 571203-78-6 | | MF: | C30H31ClN4O4 | | MW: | 547.04 | | EINECS: | | | Product Categories: | API;Inhibitors | | Mol File: | 571203-78-6.mol |  |
| | Erastin Chemical Properties |
| Boiling point | 721.9±70.0 °C(Predicted) | | density | 1.28±0.1 g/cm3(Predicted) | | storage temp. | -20°C | | solubility | DMSO: soluble5mg/mL, clear (warmed) | | pka | 5.54±0.10(Predicted) | | form | White solid | | color | white to beige | | Stability: | Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months. | | InChIKey | BKQFRNYHFIQEKN-UHFFFAOYSA-N | | SMILES | N1C2=C(C=CC=C2)C(=O)N(C2=CC=CC=C2OCC)C=1C(N1CCN(C(COC2=CC=C(Cl)C=C2)=O)CC1)C | | CAS DataBase Reference | 571203-78-6 |
| Hazard Codes | T | | Risk Statements | 25 | | Safety Statements | 45 | | RIDADR | UN 2811 6.1/PG 3 | | WGK Germany | 3 | | HS Code | 2933599590 | | Storage Class | 11 - Combustible Solids |
| | Erastin Usage And Synthesis |
| Description | Erastin, named for eradicator of RAS and small T (ST) antigen-expressing cells, is a ferroptosis inducer. It induces ferroptotic cell death in vitro, an effect that can be blocked by the ferroptosis inhibitors ciclopirox olamine, Trolox , ferrostatin-1 , U-0126 , cycloheximide , and β-mercaptoethanol. Erastin (5 μM) inhibits cystine uptake by the system xc- cystine-glutamate transporter in HT-1080 fibrosarcoma and Calu-1 lung carcinoma cells and inhibits glutamate release in an enzyme-coupled fluorescence assay (EC50 = 1.2 μM). It also selectively induces cell death in cells expressing the SV40 small T oncoprotein and oncogenic Ras (IC50s = 1.25-5 μg/ml). | | Uses | Erastin has been used:
- as a positive control for inducing ferroptosis in hepatic stellate cell (HSC)
- to induce ferroptosis and in transferrin internalization assay of human fibrosarcoma HT1080 cells
- to induce ferroptosis of muscle-derived cell lines
| | Uses | Erastin, named for eradicator of RAS and ST-expressing cells, is an irreversible antitumor agent that selectively kills cells expressing the small T oncoprotein and oncogenic Ras (IC50s = 1.25-5 μg/ml). It produces non-apoptotic tumor cell death by altering mitochondrial voltage-dependent anion channel gating, allowing cations to enter mitochondria and leading to release of oxidative species causing oxidative cell death.[Cayman Chemical] | | Definition | ChEBI: Erastin is a member of the class of quinazolines that is quinazolin-4(3H)-one in which the hydrogens at positions 2 and 3 are replaced by 1-{4-[(4-chlorophenoxy)acetyl]piperazin-1-yl}ethyl and 2-ethoxyphenyl groups, respectively. It is an inhibitor of voltage-dependent anion-selective channels (VDAC2 and VDAC3) and a potent ferroptosis inducer. It has a role as a ferroptosis inducer, an antineoplastic agent and a voltage-dependent anion channel inhibitor. It is a member of quinazolines, a member of monochlorobenzenes, an aromatic ether, a N-acylpiperazine, a N-alkylpiperazine, a diether and a tertiary carboxamide. | | General Description | Erastin is a cell-permeable piperazinyl-quinazolinone. It interacts with antiporter system Xc-. | | Biochem/physiol Actions | Erastin is an antitumor agent selective for tumor cells bearing oncogenic RAS (i.e. HRAS, KRAS). Erastin produces ferroptosis, a non-apoptotic tumor cell death, by altering mitochondrial voltage-dependent anion channel (VDAC) gating allowing cations to enter mitochondria and leading to release of oxidative species causing oxidative cell death. | | storage | Store at -20°C | | References | [1] SONAM DOLMA. Identification of genotype-selective antitumor agents using synthetic lethal chemical screening in engineered human tumor cells.[J]. Cancer Cell, 2003, 3 3: 285-296. DOI:10.1016/s1535-6108(03)00050-3
[2] SCOTT J DIXON. Pharmacological inhibition of cystine-glutamate exchange induces endoplasmic reticulum stress and ferroptosis.[J]. ACS Applied Nano Materials, 2014: e02523. DOI:10.7554/elife.02523
[3] MAMI SATO. The ferroptosis inducer erastin irreversibly inhibits system xc- and synergizes with cisplatin to increase cisplatin’s cytotoxicity in cancer cells.[J]. Scientific Reports, 2018: 968. DOI:10.1038/s41598-018-19213-4
[4] NICHOLAS YAGODA. RAS–RAF–MEK-dependent oxidative cell death involving voltage-dependent anion channels[J]. Nature, 2007, 447 7146: 865-869. DOI:10.1038/nature05859 |
| | Erastin Preparation Products And Raw materials |
|