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Erastin
cell-permeable ferroptosis activatior and antitumor agent

Catalog No.B1524
Size Price Stock Qty
10mM (in 1mL DMSO)
$165.00
In stock
5mg
$100.00
In stock
10mg
$150.00
In stock
50mg
$350.00
In stock

Tel: +1-832-696-8203

Email: [email protected]

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Sample solution is provided at 25 µL, 10mM.

Quality Control

Chemical structure

Erastin

Protocol

Cell experiment [1, 2]:

Cell lines

Engineered human tumour cells (BJ-TERT/LT/ST/RAS V12 cells), HT-1080 fibrosarcoma cell line

Preparation method

The solubility of this compound in DMSO is >27.4mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reacting condition

10 μM, 24h,

Applications

Erastin activates a rapid, oxidative, non-apoptotic cell death process. Erastin exhibits greater lethality in human tumour cells harbouring mutations in the oncogenes HRAS, KRAS or BRAF. Erastin treatment of cells harbouring oncogenic RAS causes the appearance of oxidative species and subsequent death through an oxidative, non-apoptotic mechanism. Treatment of NRAS mutant HT-1080 fibrosarcoma cells with the RSL molecule erastin (10 μM) resulted in a time-dependent increase in cytosolic and lipid ROS beginning

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1] Yagoda N, von Rechenberg M, Zaganjor E, Bauer AJ, Yang WS, Fridman DJ, Wolpaw AJ, Smukste I, Peltier JM, Boniface JJ, Smith R, Lessnick SL, Sahasrabudhe S, Stockwell BR. RAS-RAF-MEK-dependent oxidative cell death involving voltage-dependent anion channels. Nature. 2007 Jun 14;447(7146):864-8.

[2] Dixon SJ, Lemberg KM, Lamprecht MR, Skouta R, Zaitsev EM, Gleason CE, Patel DN, Bauer AJ, Cantley AM, Yang WS, Morrison B 3rd, Stockwell BR. Ferroptosis: an iron-dependent form of nonapoptotic cell death. Cell. 2012 May 25;149(5):1060-72.

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Chemical Properties

Cas No. 571203-78-6 SDF Download SDF
Chemical Name 2-[1-[4-[2-(4-chlorophenoxy)acetyl]piperazin-1-yl]ethyl]-3-(2-ethoxyphenyl)quinazolin-4-one
Canonical SMILES O=C1N(C2=CC=CC=C2OCC)C(C(N3CCN(C(COC4=CC=C(Cl)C=C4)=O)CC3)C)=NC5=C1C=CC=C5
Formula C30H31ClN4O4 M.Wt 547.04
Solubility >27.4mg/mL in DMSO Storage Store at -20°C
Shipping Condition Evaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Background

Erastin is a cell-permeable ferroptosis activatior and an antitumor agent that is selective for cell expressing oncogene RAS.

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.

In BJ-TERT/LT/ST/RASV12 cells, Erastin activated a rapid, oxidative and non-apoptotic cell death process. It exerted lethality in human cancer cells with HRAS, KRAs or BRAF oncogenic mutation involving the RAS-RAF-MEF pathway and acted via modulating VDAC (volatage-dependent anion channels). [1] In HT 1080 cells, Erastin-induced death triggered the cytosolic ROS accumulation and the induced oxidative death was iron dependent. Erastin also inhibited the activity of independent cystine/glutamate antiporter, system xc−. [2]

References:
[1] Yagoda N, von Rechenberg M, Zaganjor E, Bauer AJ, Yang WS, Fridman DJ, Wolpaw AJ, Smukste I, Peltier JM, Boniface JJ, Smith R, Lessnick SL, Sahasrabudhe S, Stockwell BR.  RAS-RAF-MEK-dependent oxidative cell death involving voltage-dependent anion channels.  Nature. 2007 Jun 14;447(7146):864-8.
[2] Dixon SJ, Lemberg KM, Lamprecht MR, Skouta R, Zaitsev EM, Gleason CE, Patel DN, Bauer AJ, Cantley AM, Yang WS, Morrison B 3rd, Stockwell BR.  Ferroptosis: an iron-dependent form of nonapoptotic cell death.  Cell. 2012 May 25;149(5):1060-72.