Cas No.: | 571203-78-6 |
Chemical Name: | Erastin |
Synonyms: | Erastin;2-[1-[4-[2-(4-chlorophenoxy)acetyl]piperazin-1-yl]ethyl]-3-(2-ethoxyphenyl)quinazolin-4-one;2-(1-{4-[2-(4-chloro-phenoxy)-acetyl]-piperazin-1-yl}-ethyl)-3-(2-ethoxy-phenyl)-3H-quinazolin-4-one;2-[1-[4-[2-(4-chlorophenoxy)acetyl]-1-piperazinyl]ethyl]-3-(2-ethoxyphenyl)-4(3H)-Quinazolinone;s7242;Erastin, >=98% (HPLC);AOB6043;HMS3653K21;BCP27907;BDBM50376126;2400AH;SB19588;AK473987;BC600677;AB009841 |
SMILES: | ClC1C([H])=C([H])C(=C([H])C=1[H])OC([H])([H])C(N1C([H])([H])C([H])([H])N(C([H])([H])C1([H])[H])C([H])(C([H])([H])[H])C1=NC2=C([H])C([H])=C([H])C([H])=C2C(N1C1=C([H])C([H])=C([H])C([H])=C1OC([H])([H])C([H])([H])[H])=O)=O |
Formula: | C30H31ClN4O4 |
M.Wt: | 547.0445 |
Purity: | 98% |
Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
Description: | Erastin is a ferroptosis activator. |
In Vivo: | Intraperitoneal injection of erastin at well-tolerated doses dramatically inhibits HT-29 xenograft growth in severe combined immunodeficient mice[3]. |
In Vitro: | Erastin triggers oxidative, iron-dependent cell death. Treatment of NRAS-mutant HT-1080 fibrosarcoma cells with the RSL molecule erastin (10 µM) results in a time-dependent increase in cytosolic and lipid ROS beginning at 2 hours[1]. Cell death triggered by erastin is significantly inhibited by antioxidants (e.g., α-tocopherol, butylated hydroxytoluene, and β-carotene) and iron chelators (e.g., deferoxamine), suggesting that ROS- and iron-dependent signaling is required for erastin-induced ferroptosis. Erastin can directly bind to VDAC2/3 in BJeLR cells. Knockdown of VDAC2 and VDAC3, but not VDAC1, leads to erastin resistance. Erastin has the ability to reduce glutathione level by directly inhibiting cystine/glutamate antiporter system Xc− activity, with activation of the ER stress response[2]. Erastin potently inhibits HT-29 cell survival. Erastin shows a dose-dependent effect, and 30 μM of erastin displays the most dramatic effect[3]. |