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Merck
CN

E7781

Erastin

≥98% (HPLC), powder, ferroptosis inducer

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

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关于此项目

经验公式（希尔记法）:
C30H31ClN4O4
化学文摘社编号:
571203-78-6
分子量:
547.04
UNSPSC Code:
12352200
PubChem Substance ID:
329799073
NACRES:
NA.77
MDL number:
MFCD09837984
Assay:
≥98% (HPLC)
Form:
powder

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产品名称

Erastin, ≥98% (HPLC)

SMILES string

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

InChI key

BKQFRNYHFIQEKN-UHFFFAOYSA-N

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

assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 5 mg/mL, clear (warmed)

storage temp.

−20°C

Gene Information

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

General description

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。

Application

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

Biochem/physiol Actions

Erastin是一种抗肿瘤药物，对携带致癌RAS的肿瘤细胞具有选择性。
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。

Features and Benefits

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。

存储类别

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

ppe

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

历史批次信息供参考:

分析证书(COA)

Lot/Batch Number
0000226790
0000226789
0000226789
0000226790
0000199817

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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
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)
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)
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
Jiao Wu et al.
Nature, 572(7769), 402-406 (2019-07-26)
Ferroptosis, a cell death process driven by cellular metabolism and iron-dependent lipid peroxidation, has been implicated in diseases such as ischaemic organ damage and cancer1,2. The enzyme glutathione peroxidase 4 (GPX4) is a central regulator of ferroptosis, and protects cells
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