Erastin
Erastin structure
|
Common Name | Erastin | ||
|---|---|---|---|---|
| CAS Number | 571203-78-6 | Molecular Weight | 547.044 | |
| Density | 1.3±0.1 g/cm3 | Boiling Point | 721.9±70.0 °C at 760 mmHg | |
| Molecular Formula | C30H31ClN4O4 | Melting Point | N/A | |
| MSDS | Chinese USA | Flash Point | 390.4±35.7 °C | |
| Symbol |
GHS06 |
Signal Word | Danger | |
Use of ErastinErastin is a ferroptosis activator. |
| Name | 2-[1-[4-[2-(4-chlorophenoxy)acetyl]piperazin-1-yl]ethyl]-3-(2-ethoxyphenyl)quinazolin-4-one |
|---|---|
| Synonym | More Synonyms |
| Description | Erastin is a ferroptosis activator. |
|---|---|
| Related Catalog | |
| 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]. |
| In Vivo | Intraperitoneal injection of erastin at well-tolerated doses dramatically inhibits HT-29 xenograft growth in severe combined immunodeficient mice[3]. |
| Cell Assay | To test erastin’s activity on colorectal cancer cell survival, HT-29 cells are treated with increasing concentrations of erastin (0.1–30 μM). MTT assay was performed[3]. |
| Animal Admin | Mice: Mice are treated daily with 10 or 30 mg/kg body weight of erastin (intraperitoneal injection, for 4 weeks) or vehicle control (Saline). Tumor volumes are calculated. Mice body weights are also recorded every week[3]. |
| References |
[2]. Xie Y, et al. Ferroptosis: process and function. Cell Death Differ. 2016 Mar;23(3):369-79. |
| Density | 1.3±0.1 g/cm3 |
|---|---|
| Boiling Point | 721.9±70.0 °C at 760 mmHg |
| Molecular Formula | C30H31ClN4O4 |
| Molecular Weight | 547.044 |
| Flash Point | 390.4±35.7 °C |
| Exact Mass | 546.203369 |
| PSA | 76.90000 |
| LogP | 4.75 |
| Appearance of Characters | white to beige |
| Vapour Pressure | 0.0±2.3 mmHg at 25°C |
| Index of Refraction | 1.634 |
| Storage condition | −20°C |
| Water Solubility | DMSO: soluble5mg/mL, clear (warmed) |
|
HSPB1 as a novel regulator of ferroptotic cancer cell death.
Oncogene 34(45) , 5617-25, (2015) Ferroptosis is an iron-dependent form of non-apoptotic cell death, but its molecular mechanism remains largely unknown. Here, we demonstrate that heat shock protein beta-1 (HSPB1) is a negative regula... |
|
|
Sensitization of acute lymphoblastic leukemia cells for LCL161-induced cell death by targeting redox homeostasis.
Biochem. Pharmacol. 105 , 14-22, (2016) Disturbed redox homeostasis with both elevated reactive oxygen species (ROS) levels and antioxidant defense mechanisms has been reported in acute lymphoblastic leukemia (ALL). We therefore hypothesize... |
|
|
Glutathione peroxidase 4 prevents necroptosis in mouse erythroid precursors.
Blood 127 , 139-48, (2016) Maintaining cellular redox balance is vital for cell survival and tissue homoeostasis because imbalanced production of reactive oxygen species (ROS) may lead to oxidative stress and cell death. The an... |
| 2-[1-[4-[2-(4-chlorophenoxy)acetyl]-1-piperazinyl]ethyl]-3-(2-ethoxyphenyl)-4(3H)-Quinazolinone |
| 2-(1-{4-[(4-Chlorophenoxy)acetyl]-1-piperazinyl}ethyl)-3-(2-ethoxyphenyl)-4(3H)-quinazolinone |
| s7242 |
| 2-(1-{4-[2-(4-chloro-phenoxy)-acetyl]-piperazin-1-yl}-ethyl)-3-(2-ethoxy-phenyl)-3H-quinazolin-4-one |
| 2-(1-{4-[(4-chlorophenoxy)acetyl]piperazin-1-yl}ethyl)-3-(2-ethoxyphenyl)quinazolin-4(3H)-one |
| 4(3H)-Quinazolinone, 2-[1-[4-[2-(4-chlorophenoxy)acetyl]-1-piperazinyl]ethyl]-3-(2-ethoxyphenyl)- |
| Erastin |