化合物 Erastin|T1765

價(jià)格	￥415
包裝	1mg

最小起訂量	1mg
發(fā)貨地	上海
更新日期	2024-12-02

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產(chǎn)品詳情

中文名稱(chēng):化合物 Erastin	英文名稱(chēng):Erastin
CAS:571203-78-6	品牌: TargetMol
產(chǎn)地: 美國(guó)	保存條件: Powder: -20°C for 3 years \| Shipping with blue ice.
純度規(guī)格: 99.75%	產(chǎn)品類(lèi)別: 抑制劑
貨號(hào): T1765

Product Introduction

Bioactivity

名稱(chēng)	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.
細(xì)胞實(shí)驗(yàn)	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].
動(dòng)物實(shí)驗(yàn)	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].
體外活性	方法：人胃癌細(xì)胞 HGC-27 用 Erastin (1-50 μM) 處理 24 h，使用 CCK-8 方法檢測(cè)細(xì)胞生長(zhǎng)抑制情況。結(jié)果：Erastin 劑量依賴(lài)性地抑制 HGC-27 細(xì)胞生長(zhǎng)，IC50 約為 14.39 μM。[1] 方法：人黑色素瘤細(xì)胞 A375 用 Erastin (2-10 μM) 處理 3-12 h，使用 Western Blot 方法檢測(cè)靶點(diǎn)蛋白表達(dá)水平。結(jié)果：Erastin 處理引起 A375 細(xì)胞中 VDAC2 和 VDAC3 的水平顯著下調(diào)，VDAC1 的水平略有降低。[2] 方法：人結(jié)腸癌細(xì)胞 HT-29 用 Erastin (0.1-30 μM) 處理 12 h，使用 Flow Cytometry 方法檢測(cè)細(xì)胞內(nèi) ROS 水平。結(jié)果：Erastin 處理顯著增加了 HT-29 細(xì)胞中的 ROS水平。[3]
體內(nèi)活性	方法：為檢測(cè)體內(nèi)抗腫瘤活性，將 Erastin (20 mg/kg in 20 μL DMSO plus 130 μL corn oil) 腹腔注射給攜帶人前列腺癌腫瘤 DU145、ARCaP、PC3 或 H660 的 NSG 小鼠，每天一次，持續(xù)二至五周。結(jié)果：Erastin 治療顯著抑制人前列腺癌腫瘤的生長(zhǎng)，表明在體內(nèi)具有抗腫瘤活性。[4] 方法：為研究 Erastin 治療對(duì)抗癌輻射效率的影響，將 Erastin (15 mg/kg in 5% DMSO/corn oil) 腹腔注射給攜帶人肺腺癌腫瘤 NCI-H1975 的 BALB/c Slc-nu/nu 小鼠，每天一次，持續(xù)三天。在最后一次注射 Erastin 后 24 h，用 3 Gy 的 X 射線局部照射麻醉的小鼠。結(jié)果：Erastin 治療的 NCI-H1975 細(xì)胞移植小鼠顯示出對(duì) X 射線照射的增敏趨勢(shì)，同時(shí)腫瘤內(nèi)谷胱甘肽濃度降低。[5]
存儲(chǔ)條件	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)
關(guān)鍵字	Ferroptosis \| VDAC \| Voltage-dependent anion channel \| Erastin \| inhibit \| Inhibitor
相關(guān)產(chǎn)品	L-Cystine \| Coenzyme Q10 \| L-Glutamic acid \| L-Glutamic acid monosodium salt \| Artemisinin \| Curcumin \| α-Vitamin E \| Butylated hydroxytoluene \| L-Glutamine \| Sorafenib \| Acetylcysteine \| TBHQ

關(guān)鍵字： Erastin|TargetMol

公司簡(jiǎn)介

上海陶術(shù)生物科技有限公司為美國(guó)Target Molecule Corp. ( Target Mol ) 在上海建立的全資子公司。我們與美國(guó)波士頓、德國(guó)慕尼黑的同事一起，為北美、歐洲和亞洲從事藥物研發(fā)和生物學(xué)研究的科學(xué)家提供優(yōu)質(zhì)的產(chǎn)品和專(zhuān)業(yè)的服務(wù)。公司下設(shè)篩選事業(yè)部，化學(xué)事業(yè)部，生物事業(yè)部和新材料部。從虛擬篩選到實(shí)體化合物分子供應(yīng)；從商業(yè)化產(chǎn)品銷(xiāo)售到個(gè)性化定制合成；從對(duì)明確靶點(diǎn)的分子篩選到對(duì)明確分子的多靶點(diǎn)篩選，從高通量篩選到化學(xué)結(jié)構(gòu)優(yōu)化，我們都可以滿(mǎn)足您的科研用品及技術(shù)服務(wù)的需求。經(jīng)過(guò)在中國(guó)市場(chǎng)五年的精心耕耘，我們已成為篩選化合物領(lǐng)域優(yōu)秀的供應(yīng)商，為超過(guò)五百家學(xué)校和各類(lèi)企業(yè)提供了品質(zhì)卓越的小分子化合物和藥物篩

成立日期	2013-04-18 （12年）	注冊(cè)資本	566.2651萬(wàn)人民幣
員工人數(shù)	100-500人	年?duì)I業(yè)額	￥ 1億以上
主營(yíng)行業(yè)	化學(xué)試劑,生物活性小分子	經(jīng)營(yíng)模式	貿(mào)易,試劑,定制,服務(wù)

TargetMol中國(guó)（陶術(shù)生物）

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公司成立：12年
注冊(cè)資本：566.2651萬(wàn)人民幣
企業(yè)類(lèi)型：有限責(zé)任公司(自然人投資或控股)
主營(yíng)產(chǎn)品：小分子抑制劑，藥物篩選化合物庫(kù)，天然產(chǎn)物，活性分子化合物等
公司地址：上海市閘北區(qū)江場(chǎng)三路28號(hào)4樓

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