化合物 Erastin|T1765

Erastin
571203-78-6

￥415 1mg 起订

上海更新日期：2024-09-14

TargetMol中国（陶术生物）

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联系人：邵小姐

电话：021-021-33632979拨打

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邮箱：marketing@targetmol.com

产品详情:

中文名称：: 化合物 Erastin

英文名称：: Erastin

CAS号：: 571203-78-6

品牌：: TargetMol

产地：: 美国

保存条件：: Powder: -20°C for 3 years | Shipping with blue ice.

纯度规格：: 99.75%

产品类别：: 抑制剂

货号：: T1765

Product Introduction

Bioactivity

名称	Erastin
描述	Erastin is an iron death activator that acts on the mitochondrial VDAC in a ROS- and iron-dependent manner. Erastin has anti-tumor activity and acts selectively on tumor cells with RAS-carcinogenic mutations.
细胞实验	BJeLR cells were plated at 100,000 cells/dish in 35 mm tissue culture dishes. After 12h cells were treated with vehicle (DMSO; 10 hrs), erastin (37 μM; 10 hrs), staurosporine (750 nM; 8 hrs), hydrogen peroxide (16 mM; 1 hr) or rapamycin (100 nM; 24 hrs). Cells were fixed with 2.5% glutaraldehyde in 0.1 M Sorenson's buffer (0.1 M H2PO4, 0.1 M HPO4 (pH 7.2)) for at least 1 h, and then treated with 1% OsO4 in 0.1 M Sorenson's buffer for 1 h. Enblock staining used 1% tannic acid. After dehydration through an ethanol series, cells were embedded in Lx-112 and Embed-812 (EMS). Thin sections were cut on an MT-7000 ultramicrotome, stained with 1% uranyl acetate and 0.4% lead citrate, and examined under a Jeol JEM-1200 EXII electron microscope. Pictures were taken on an ORCA-HR digital camera at 5,000-50,000-fold magnification [1].
动物实验	Tumor growth studies were performed in severe combined immunodeficient (SCID) mice xenograft model. Briefly, 2×10^6 viable HT-29 cells in 100 μL of growth medium (per mouse) were subcutaneously inoculated, and mice bearing ~100 mm3 tumors were randomly divided into three groups with 10 mice per group. Mice were treated daily with 10 or 30 mg/kg body weight of erastin (intraperitoneal injection, for 4 weeks) or vehicle control (Saline). Tumor volumes were calculated by the modified ellipsoid formula: (π / 6) ×AB2, where A is the longest and B is the shortest perpendicular axis of a tumor mass. Mice body weights were also recorded every week. Humane endpoints were always utilized to minimize mice suffering. Animals were observed on daily bases. Signs such as significant-reduced locomotion, severe diarrhea, severe piloerection or a sudden weight loss (> 20%) were recorded. If animals reached these endpoints they were euthanized by exsanguination under 2,2,2-tribromoethanol anesthesia (4 mg/10 g body weight). All injections were performed under the 2,2,2-tribromoethanol anesthesia method [3].
体外活性	方法：人胃癌细胞 HGC-27 用 Erastin (1-50 μM) 处理 24 h，使用 CCK-8 方法检测细胞生长抑制情况。结果：Erastin 剂量依赖性地抑制 HGC-27 细胞生长，IC50 约为 14.39 μM。[1] 方法：人黑色素瘤细胞 A375 用 Erastin (2-10 μM) 处理 3-12 h，使用 Western Blot 方法检测靶点蛋白表达水平。结果：Erastin 处理引起 A375 细胞中 VDAC2 和 VDAC3 的水平显著下调，VDAC1 的水平略有降低。[2] 方法：人结肠癌细胞 HT-29 用 Erastin (0.1-30 μM) 处理 12 h，使用 Flow Cytometry 方法检测细胞内 ROS 水平。结果：Erastin 处理显著增加了 HT-29 细胞中的 ROS水平。[3]
体内活性	方法：为检测体内抗肿瘤活性，将 Erastin (20 mg/kg in 20 μL DMSO plus 130 μL corn oil) 腹腔注射给携带人前列腺癌肿瘤 DU145、ARCaP、PC3 或 H660 的 NSG 小鼠，每天一次，持续二至五周。结果：Erastin 治疗显著抑制人前列腺癌肿瘤的生长，表明在体内具有抗肿瘤活性。[4] 方法：为研究 Erastin 治疗对抗癌辐射效率的影响，将 Erastin (15 mg/kg in 5% DMSO/corn oil) 腹腔注射给携带人肺腺癌肿瘤 NCI-H1975 的 BALB/c Slc-nu/nu 小鼠，每天一次，持续三天。在最后一次注射 Erastin 后 24 h，用 3 Gy 的 X 射线局部照射麻醉的小鼠。结果：Erastin 治疗的 NCI-H1975 细胞移植小鼠显示出对 X 射线照射的增敏趋势，同时肿瘤内谷胱甘肽浓度降低。[5]
存储条件	Powder: -20°C for 3 years \| Shipping with blue ice.
溶解度	DMSO : 6.43 mg/mL (11.75 mM), The compound is unstable in solution. Please use soon. Ethanol : < 1 mg/mL (insoluble or slightly soluble) 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 1.6 mg/mL (2.92 mM), Please add co-solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. H2O : < 1 mg/mL (insoluble or slightly soluble)
关键字	Ferroptosis \| VDAC \| Voltage-dependent anion channel \| Erastin \| inhibit \| Inhibitor
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Erastin|TargetMol

上海陶术生物科技有限公司为美国Target Molecule Corp. ( Target Mol ) 在上海建立的全资子公司。我们与美国波士顿、德国慕尼黑的同事一起，为北美、欧洲和亚洲从事药物研发和生物学研究的科学家提供优质的产品和专业的服务。公司下设筛选事业部，化学事业部，生物事业部和新材料部。从虚拟筛选到实体化合物分子供应；从商业化产品销售到个性化定制合成；从对明确靶点的分子筛选到对明确分子的多靶点筛选，从高通量筛选到化学结构优化，我们都可以满足您的科研用品及技术服务的需求。经过在中国市场五年的精心耕耘，我们已成为筛选化合物领域优秀的供应商，为超过五百家学校和各类企业提供了品质卓越的小分子化合物和药物筛

成立日期	(12年)
注册资本	566.2651万人民币
员工人数	100-500人
年营业额	￥ 1亿以上
经营模式	贸易,试剂,定制,服务
主营行业	化学试剂,生物活性小分子