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Merck
CN
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文件

E7781

Sigma-Aldrich

Erastin

≥98% (HPLC)

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别名:
2-[1-[4-[2-（4-氯苯氧基）乙酰基]-1-哌嗪基]乙基]-3-（2-乙氧基苯基）-4-（3H）喹唑啉酮
经验公式（希尔记法）:
C30H31ClN4O4
CAS号:
571203-78-6
分子量:
547.04
MDL编号:
MFCD09837984
UNSPSC代码:
12352200
PubChem化学物质编号:
329799073
NACRES:
NA.77

检测方案

≥98% (HPLC)

形式

powder

颜色

white to beige

溶解性

DMSO: 5 mg/mL, clear (warmed)

储存温度

−20°C

SMILES字符串

CCOc1ccccc1N2C(=O)c3ccccc3N=C2C(C)N4CCN(CC4)C(=O)COc5ccc(Cl)cc5

InChI

1S/C30H31ClN4O4/c1-3-38-27-11-7-6-10-26(27)35-29(32-25-9-5-4-8-24(25)30(35)37)21(2)33-16-18-34(19-17-33)28(36)20-39-23-14-12-22(31)13-15-23/h4-15,21H,3,16-20H2,1-2H3

InChI key

BKQFRNYHFIQEKN-UHFFFAOYSA-N

基因信息

human ... hRas(3265)
mouse ... hRas(15461)
rat ... hRas(293621)

一般描述

爱拉斯汀是一种细胞可透过性哌嗪基-喹唑啉酮。它与逆向转运系统Xc-相互作用。

应用

爱拉斯汀已用于：
  • 肝星状细胞(HSC)中诱导铁死亡的阳性对照
  • 诱导铁死亡及人纤维肉瘤HT1080细胞转铁蛋白内化测定
  • 诱导肌肉来源细胞系铁死亡

生化/生理作用

Erastin是一种针对携带致癌RAS（即HRAS，KRAS）的肿瘤细胞的选择性抗肿瘤剂。Erastin可通过改变线粒体电压依赖性阴离子通道（VDAC）门控产生铁死亡（一种非凋亡性肿瘤细胞死亡），从而允许阳离子进入线粒体并导致氧化物质释放，进而导致氧化细胞死亡。

特点和优势

该化合物是细胞凋亡研究的推荐产品。点击此处，了解更多精选的细胞凋亡产品。了解更多有关用于其他研究领域的生物活性小分子的信息，请访问 sigma.com/discover-bsm。

WGK

WGK 3

闪点(°F)

Not applicable

闪点(°C)

Not applicable

个人防护装备

Eyeshields, Faceshields, Gloves, type P2 (EN 143) respirator cartridges

分析证书(COA)

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Nicholas Yagoda et al.
Nature, 447(7146), 864-868 (2007-06-15)
Therapeutics that discriminate between the genetic makeup of normal cells and tumour cells are valuable for treating and understanding cancer. Small molecules with oncogene-selective lethality may reveal novel functions of oncoproteins and enable the creation of more selective drugs. Here
Cell growth potential drives ferroptosis susceptibility in rhabdomyosarcoma and myoblast cell lines
Codenotti S, et al.
Journal of Cancer Research and Clinical Oncology, 144(9), 1717-1730 (2018)
Sonam Dolma et al.
Cancer cell, 3(3), 285-296 (2003-04-05)
We used synthetic lethal high-throughput screening to interrogate 23,550 compounds for their ability to kill engineered tumorigenic cells but not their isogenic normal cell counterparts. We identified known and novel compounds with genotype-selective activity, including doxorubicin, daunorubicin, mitoxantrone, camptothecin, sangivamycin
The ferroptosis inducer erastin promotes proliferation and differentiation in human peripheral blood mononuclear cells
Wang D, et al.
Biochemical and Biophysical Research Communications, 503(3), 1689-1695 (2018)
Antonio Bruni et al.
Cell death & disease, 9(6), 595-595 (2018-05-24)
Human islet transplantation has been hampered by donor cell death associated with the islet preparation procedure before transplantation. Regulated necrosis pathways are biochemically and morphologically distinct from apoptosis. Recently, ferroptosis was identified as a non-apoptotic form of iron-dependent regulated necrosis
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