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Erastin

现货
Catalog No.
B1524
Ferroptosis激活剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 1,650.00
现货
5mg
¥ 1,000.00
现货
10mg
¥ 1,500.00
现货
50mg
¥ 3,500.00
现货

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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.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt547.04
Cas No.571203-78-6
FormulaC30H31ClN4O4
Solubility≥10.92mg/mL in DMSO with gentle warming
Chemical Name2-[1-[4-[2-(4-chlorophenoxy)acetyl]piperazin-1-yl]ethyl]-3-(2-ethoxyphenyl)quinazolin-4-one
SDFDownload SDF
Canonical SMILESO=C1N(C2=CC=CC=C2OCC)C(C(N3CCN(C(COC4=CC=C(Cl)C=C4)=O)CC3)C)=NC5=C1C=CC=C5
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

细胞实验 [1, 2]:

溶解方法

工程化人类肿瘤细胞(BJ-TERT/LT/ST/RAS V12细胞),HT-1080纤维肉瘤细胞系

反应条件

该化合物在DMSO中的溶解度大于27.4 mg/mL。若获取更高浓度的溶液,可在37℃下孵育10分钟,随后在超声波浴中摇匀。-20℃以下可储存数月。

应用

10 μM,24h

溶解方法

Erastin激活快速、氧化及非凋亡细胞死亡过程。在致癌基因HRAS、KRAS或BRAF突变的人类肿瘤细胞中,Erastin表现出更大的致死性。在携带致癌RAS的细胞中,Erastin导致氧化物质的出现,随后通过氧化及非凋亡机制死亡。在NRAS突变HT-1080纤维肉瘤细胞中,RSL分子Erastin(10 μM)处理以时间依赖性方式增加细胞溶质和脂质ROS的起始。

注意事项

由于实验环境的不同,实际溶解度可能与理论值略有不同,请测试室内所有化合物的溶解度。

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.

质量控制

化学结构

Erastin