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Erastin

Erastin

产品编号 T1765   CAS 571203-78-6

Erastin 是一种作用于线粒体 VDAC 的铁死亡激活剂,具有 ROS 和铁依赖性。Erastin 具有抗肿瘤活性,选择性作用于 RAS 致癌突变的肿瘤细胞。该产品在溶液中不稳定,建议现配现用。

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Erastin Chemical Structure
Erastin, CAS 571203-78-6
规格 价格/CNY 货期 数量
1 mg ¥ 415 现货
1 mg * 5 ¥ 998 现货
1 mg * 10 ¥ 1,673 现货
1 mg * 25 ¥ 3,325 现货
1 mg * 50 ¥ 5,551 现货
产品目录号及名称: Erastin (T1765)
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选择批次  
纯度: 99.75%
纯度: 99.6%
纯度: 99.59%
纯度: 99.22%
纯度: 99.18%
纯度: 98.48%
纯度: 98%
纯度: 98%
更多批次查询请联系客服
生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 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. The product is unstable in solution and is recommended to be dispensed now.
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]
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].
化合物与蛋白结合的复合物

T1765_1

Overall structure of Erastin-bound xCT-4F2hc complex

分子量 547.04
分子式 C30H31ClN4O4
CAS No. 571203-78-6

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 16 mg/mL (29.2 mM), The compound is unstable in solution and is recommended to be prepared and used immediately.

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

H2O: < 1 mg/mL (insoluble or slightly soluble)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.828 mL 9.1401 mL 18.2802 mL 45.7005 mL
5 mM 0.3656 mL 1.828 mL 3.656 mL 9.1401 mL
10 mM 0.1828 mL 0.914 mL 1.828 mL 4.57 mL
20 mM 0.0914 mL 0.457 mL 0.914 mL 2.285 mL

计算器

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参考文献

1. Sun Y, et al. Erastin induces apoptotic and ferroptotic cell death by inducing ROS accumulation by causing mitochondrial dysfunction in gastric cancer cell HGC‑27. Mol Med Rep. 2020 Oct;22(4):2826-2832. 2. Yang Y, et al. Nedd4 ubiquitylates VDAC2/3 to suppress erastin-induced ferroptosis in melanoma. Nat Commun. 2020 Jan 23;11(1):433. 3. Huo H, et al. Erastin Disrupts Mitochondrial Permeability Transition Pore (mPTP) and Induces Apoptotic Death of Colorectal Cancer Cells. PLoS One. 2016 May 12;11(5):e0154605. 4. Ghoochani A, et al. Ferroptosis Inducers Are a Novel Therapeutic Approach for Advanced Prostate Cancer. Cancer Res. 2021 Mar 15;81(6):1583-1594. 5. Shibata Y, et al. Erastin, a ferroptosis-inducing agent, sensitized cancer cells to X-ray irradiation via glutathione starvation in vitro and in vivo. PLoS One. 2019 Dec 4;14(12):e0225931. 6. Yan B, Ai Y, Sun Q, et al. Membrane Damage during Ferroptosis Is Caused by Oxidation of Phospholipids Catalyzed by the Oxidoreductases POR and CYB5R1[J]. Molecular Cell. 2020

文献引用

1. Hu G, Cui Z, Chen X, et al.Suppressing Mesenchymal Stromal Cell Ferroptosis Via Targeting a Metabolism‐Epigenetics Axis Corrects their Poor Retention and Insufficient Healing Benefits in the Injured Liver Milieu.Advanced Science.2023: 2206439. 2. Li Y, Yang W, Zheng Y, et al.Targeting fatty acid synthase modulates sensitivity of hepatocellular carcinoma to sorafenib via ferroptosis.Journal of Experimental & Clinical Cancer Research.2023, 42(1): 1-19. 3. Xiang P, Chen Q, Chen L, et al.Metabolite Neu5Ac triggers SLC3A2 degradation promoting vascular endothelial ferroptosis and aggravates atherosclerosis progression in ApoE-/-mice.Theranostics.2023, 13(14): 4993. 4. Chen C, Yang Y, Guo Y, et al.CYP1B1 inhibits ferroptosis and induces anti-PD-1 resistance by degrading ACSL4 in colorectal cancer.Cell Death & Disease.2023, 14(4): 271. 5. Zeng S T, Shao W, Yu Z Y, et al.Construction of a TICT-AIE-Integrated Unimolecular Platform for Imaging Lipid Droplet–Mitochondrion Interactions in Live Cells and In Vivo.ACS Sensors.2022 6. Zhu X, Huang N, Ji Y, et al.Brusatol induces ferroptosis in oesophageal squamous cell carcinoma by repressing GSH synthesis and increasing the labile iron pool via inhibition of the NRF2 pathway.Biomedicine & Pharmacotherapy.2023, 167: 115567. 7. Zhao G, Liang J, Shan G, et al.KLF11 regulates lung adenocarcinoma ferroptosis and chemosensitivity by suppressing GPX4.Communications Biology.2023, 6(1): 570. 8. Wang Y, Li B, Liu G, et al.Corilagin attenuates intestinal ischemia/reperfusion injury in mice by inhibiting ferritinophagy-mediated ferroptosis through disrupting NCOA4-ferritin interaction.Life Sciences.2023: 122176. 9. Bow Y D, Ko C C, Chang W T, et al.A novel quinoline derivative, DFIQ, sensitizes NSCLC cells to ferroptosis by promoting oxidative stress accompanied by autophagic dysfunction and mitochondrial damage.Cancer Cell International.2023, 23(1): 1-11. 10. Gartzke L P, Hendriks K D W, Hoogstra-Berends F, et al.Inhibition of Ferroptosis Enables Safe Rewarming of HEK293 Cells following Cooling in University of Wisconsin Cold Storage Solution.International Journal of Molecular Sciences.2023, 24(13): 10939.
11. Jiang X, Teng X, Shi H, et al.Discovery and optimization of olanzapine derivatives as new ferroptosis inhibitors.Bioorganic Chemistry.2023: 106393. 12. Liu J, Meng F, Lv J, et al.Comprehensive Monitoring of Mitochondrial Viscosity Variation during Different Cell Death Processes by a NIR Mitochondria-targeting Fluorescence Probe.Spectrochimica Acta Part A: Molecular and Biomolecular Spectroscopy.2023: 122602. 13. Tian Q, Zhou Y, Zhu L, et al. Development and validation of a ferroptosis-related gene signature for overall survival prediction in lung adenocarcinoma. Frontiers in Cell and Developmental Biology. 2021, 9. 14. Yan R, Xie E, Li Y, et al. The structure of erastin-bound xCT–4F2hc complex reveals molecular mechanisms underlying erastin-induced ferroptosis. Cell Research. 2022-32(7)P1-4 15. Kong R, Wang N, Han W, et al. IFNγ‐mediated repression of system xc− drives vulnerability to induced ferroptosis in hepatocellular carcinoma cells. Journal of Leukocyte Biology. 2021, 110(2): 301-314. 16. Zheng Y, Kong F, Liu S, et al. Membrane protein-chimeric liposome-mediated delivery of triptolide for targeted hepatocellular carcinoma therapy. Drug delivery. 2021 17. Tan Q, Fang Y, Peng X, et al. A new ferroptosis inhibitor, isolated from Ajuga nipponensis, protects neuronal cells via activating NRF2-antioxidant response elements (AREs) pathway. Bioorganic Chemistry. 2021: 105177. 18. Zhou Y, Wu H, Wang F, et al. GPX7 Is Targeted by miR-29b and GPX7 Knockdown Enhances Ferroptosis Induced by Erastin in Glioma. Frontiers in oncology. 2021, 11: 802124-802124. 19. Peng X, Tan Q, Wu L, et al. Ferroptosis Inhibitory Aromatic Abietane Diterpenoids from Ajuga decumbens and Structural Revision of Two 3, 4-Epoxy Group-Containing Abietanes. Journal of Natural Products. 2022 20. Li H, Shi W, Li X, et al. Ferroptosis is Accompanied by• OH Generation and Cytoplasmic Viscosity Increase Revealed via Dual-Functional Fluorescence Probe. Journal of the American Chemical Society. 2019 21. Zhu, Lizhe, et al. A novel ferroptosis-related gene signature for overall survival prediction in patients with breast cancer. Frontiers in Cell and Developmental Biology. 9 (2021) 22. Ning X, Qi H, Yuan Y, et al. Identification of a new small molecule that initiates ferroptosis in cancer cells by inhibiting the system Xc− to deplete GSH. European Journal of Pharmacology. 2022: 175304. 23. Kong R, Wang N, Han W, et al. IFNγ‐mediated repression of system xc− drives vulnerability to induced ferroptosis in hepatocellular carcinoma cells. Journal of Leukocyte Biology. 2021, 110(2): 301-314. 24. Bi G, Liang J, Zhao M, et al. MiR-6077 promotes cisplatin/pemetrexed resistance in lung adenocarcinoma by targeting CDKN1A/cell cycle arrest and KEAP1/ferroptosis pathways. Molecular Therapy-Nucleic Acids. 2022 25. Yan B, Ai Y, Sun Q, et al. Membrane Damage during Ferroptosis Is Caused by Oxidation of Phospholipids Catalyzed by the Oxidoreductases POR and CYB5R1. Molecular Cell. 2020 26. Fang Y, Tan Q, Zhou H, et al. Discovery and optimization of 2-(trifluoromethyl) benzimidazole derivatives as novel ferroptosis inducers in vitro and in vivo. European Journal of Medicinal Chemistry. 2022: 114905. 27. Li P, Lin Q, Sun S, et al. Inhibition of cannabinoid receptor type 1 sensitizes triple-negative breast cancer cells to ferroptosis via regulating fatty acid metabolism. Cell Death & Disease. 2022, 13(9): 1-15. 28. Li H, Shi W, Li X, et al. Ferroptosis Accompanied by •OH Generation and Cytoplasmic Viscosity Increase Revealed via Dual-Functional Fluorescence Probe. Journal of the American Chemical Society. 2019, 141(45): 18301-18307 29. Wu Z, Geng Y, Lu X, et al. Chaperone-mediated autophagy is involved in the execution of ferroptosis. Proceedings of the National Academy of Sciences. 2019 Feb 19;116(8):2996-3005 30. Wang J, Yan J T, Zeng S T, et al.Revealing Mitochondrion–Lysosome Dynamic Interactions and pH Variations in Live Cells with a pH-Sensitive Fluorescent Probe.Analytical Chemistry.2023 31. Li Z, Zhao B, Zhang Y, et al.Mitochondria-mediated ferroptosis contributes to the inflammatory responses of bovine viral diarrhea virus (BVDV) in vitro.Journal of Virology.2024: e01880-23. 32. Yang X, Li W, Li S, et al.Fish oil-based microemulsion can efficiently deliver oral peptide blocking PD-1/PD-L1 and simultaneously induce ferroptosis for cancer immunotherapy.Journal of Controlled Release.2024, 365: 654-667. 33. Yin Z, Liu Q, Gao Y, et al.GOLPH3 promotes tumor malignancy via inhibition of ferroptosis by upregulating SLC7A11 in cholangiocarcinoma.Molecular Carcinogenesis.2024 34. Du Y, Zhou Y, Yan X, et al.APE1 inhibition enhances ferroptotic cell death and contributes to hepatocellular carcinoma therapy.Cell Death & Differentiation.2024: 1-16. 35. Tan Q, Wu D, Lin Y, et al.Identifying eleven new ferroptosis inhibitors as neuroprotective agents from FDA-approved drugs.Bioorganic Chemistry.2024: 107261.
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Matrine Setanaxib CIL56 Sorafenib Bay 11-7085 PD146176 ROS-generating agent 1 Vildagliptin

相关化合物库

该产品包含在如下化合物库中:
抗癌临床化合物库 抗癌活性化合物库 抗癌药物库 铁死亡化合物库 血液病分子库 抗衰老化合物库 NO PAINS 化合物库 已知活性化合物库 线粒体靶向库 经典已知活性库

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请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。

体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

第一步:请输入动物实验的基本信息
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您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

Erastin 571203-78-6 Apoptosis Membrane transporter/Ion channel Ferroptosis VDAC Voltage-dependent anion channel inhibit Inhibitor inhibitor

 

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