Erastin

Catalog No.S7242

Erastin is a ferroptosis activator by acting on mitochondrial VDAC, exhibiting selectivity for tumor cells bearing oncogenic RAS.

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Erastin Chemical Structure

Erastin Chemical Structure
Molecular Weight: 547.04

Validation & Quality Control

2 customer reviews :

Quality Control & MSDS

Product Information

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Product Description

Biological Activity

Description Erastin is a ferroptosis activator by acting on mitochondrial VDAC, exhibiting selectivity for tumor cells bearing oncogenic RAS.
Targets Ferroptosis [1]
In vitro Erastin is selectively lethal to oncogenic RAS-mutant cell lines, and triggers a unique iron-dependent form of non-apoptotic cell death called ferroptosis. [1] [2] Erastin binds directly to VDAC2 and causes mitochondrial damage via ROS production in an NADH-dependent manner, which induces cell death in some tumor cells harbouring activating mutations in the RAS-RAF-MEK pathway. [3] In addition, erastin, via inducing ROS-mediated CID (Caspase-independent cell death), strongly enhances the effect of cisplatin in WT EGFR cells. [4]
In vivo
Features

Protocol(Only for Reference)

Cell Assay: [1]

Cell lines BJ-TERT/LT/ST/RASV12 cells
Concentrations 5 or 10 μg/mL
Incubation Time 6-11 hours
Method BJ-TERT/LT/ST/RASV12 cells are seeded in 100 mm dishes and allowed to grow overnight. Cells are treated with erastin (5 or 10 μg/ml) for 6, 8, or 11 hr. A camptothecin-treated (0.4 μg/ml) control is maintained, treated at the time of seeding for 20 hours. After the treatment, cells are harvested with trypsin/EDTA and washed once with fresh medium containing serum and then twice with phosphate-buffered saline. Cells are resuspended in 1× binding buffer. 100 μL is incubated with 5 μL of Annexin V-FITC and propidium iodiode for 15 min in the dark at room temperature. Then 400 μl of the 1× binding buffer s added and the cells analyzed by flow cytometry. Data are acquired and analyzed using Cellquest software. Only viable cells that do not stain with propidium iodiode are analzyed for Annexin V-FITC staining using the FL1 channel.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] Dolma S, et al. Cancer Cell. 2003, 3(3), 285-296.

[2] Dixon SJ, et al. Cell. 2012, 149(5), 1060-1072.

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Chemical Information

Download Erastin SDF
Molecular Weight (MW) 547.04
Formula

C30H31ClN4O4

CAS No. 571203-78-6
Storage 3 years -20℃powder
6 months-80℃in solvent
Synonyms N/A
Solubility (25°C) * In vitro DMSO 19 mg/mL (34.73 mM)
Water <1 mg/mL (<1 mM)
Ethanol <1 mg/mL (<1 mM)
In vivo 5% DMSO+corn oil 2.5mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Name 4(3H)-Quinazolinone, 2-[1-[4-[2-(4-chlorophenoxy)acetyl]-1-piperazinyl]ethyl]-3-(2-ethoxyphenyl)-

Customer Product Validation(2)


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Rating
Source Oncogene, 2015, 10.1038/onc.2015.32. Erastin purchased from Selleck
Method Western Blot
Cell Lines HeLa、 U2OS、LNCaP cells
Concentrations 0.5、5、5 µM
Incubation Time 24 h
Results Western blot analysis revealed that the protein level of HSPB1, but not HSP90 and HSP70, was significantly increased in HeLa cells following erastin treatment. In addition, erastin also induced the expression of HSPB1, but not HSP90 and HSP70, in U2OS and LNCaP.

Click to enlarge
Rating
Source Oncogene, 2015, 10.1038/onc.2015.32. Erastin purchased from Selleck
Method Western Blot
Cell Lines HeLa cells
Concentrations 0.5 µM
Incubation Time 24 h
Results In response to erastin, the levels of phosphorylation and expression of HSPB1 were elevated in HeLa cells.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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