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Etoposide

Etoposide

产品编号 T0132   CAS 33419-42-0
别名: VP-16, 依托泊苷, 依托泊甙, VP-16-213

Etoposide (VP-16-213) 是一种拓扑异构酶 II 的抑制剂,通过与拓扑异构酶 II 和 DNA 形成复合物来抑制 DNA 合成 (IC50=60.3 μM)。Etoposide 具有抗肿瘤活性,可以诱导细胞凋亡自噬

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Etoposide Chemical Structure
Etoposide, CAS 33419-42-0
规格 价格/CNY 货期 数量
50 mg ¥ 287 现货
100 mg ¥ 430 现货
200 mg ¥ 697 现货
500 mg ¥ 1,650 现货
1 mL * 10 mM (in DMSO) ¥ 450 现货
产品目录号及名称: Etoposide (T0132)
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纯度: 99.94%
纯度: 99.93%
纯度: 99.19%
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天然产物信息
生物活性
化学信息
存储 & 溶解度
参考文献
植物来源
结构类型
产品描述 Etoposide (VP-16-213) is a topoisomerase II inhibitor that inhibits DNA synthesis by forming a complex with topoisomerase II and DNA (IC50=60.3 μM). Etoposide has antitumor activity and induces apoptosis and autophagy.
靶点活性 Topo II:60.3 μM
体外活性 方法:人宫颈癌细胞 HeLa 用 Etoposide (25-400 μM) 处理 24-48 h,使用 MTT 方法检测细胞活力。
结果:Etoposide 抑制 Hela 细胞增殖,处理 24 h 和 48 h 的 IC50 分别为 167.3 μM 和 52.7
μM。[1]
方法:人肺腺癌细胞 A549 用 Etoposide (0.75-3 μM) 处理 4 h,使用 Flow Cytometry 方法检测细胞周期情况。
结果:Etoposide 导致 G0/G1 和 S 期的 A549 细胞百分比显著降低。同时,G2/M 期的细胞显著增加。[2]
方法:小鼠胚胎成纤维细胞 MEFs 用 Etoposide (1.5-150 μM) 处理 3-18 h,使用 Western Blot 方法检测靶点蛋白表达水平。
结果:150 μM的 Etoposide 在 6 h 内诱导 Caspase-3 的强烈裂解,而 1.5 或 15 μM 仅在 18 h 后激活 Caspase-3。[3]
体内活性 方法:为检测体内抗肿瘤活性,将 Etoposide (10 mg/kg) 和 Cisplatin (5-7.5 mg/kg) 腹腔注射给携带人子宫内膜腺癌肿瘤 Ishikawa 的 KSN nude 小鼠,每两天一次,持续两周。
结果:作为单一药物,Etoposide 对肿瘤生长几乎没有抑制作用。Etoposide 和 Cisplatin 联合治疗显著抑制肿瘤生长。[4]
方法:为检测体内抗肿瘤活性,将 Etoposide (80 mg/kg in 0.5% methylcellulose) 灌胃给药给携带人胶质母细胞肿瘤 U87 的免疫缺陷小鼠,每天一次,持续四十天。
结果:80 mg/kg Etoposide 抑制 U87 肿瘤生长,抑制率为95%。[5]
激酶实验 Nuclear extracts are prepared, and nuclei are isolated. The activity of topoisomerase II is calculated from the percentage of decatenation obtained. Tritiated kinoplast DNA (KDNA 0.22 μg) is used as a substrate. Etoposide and topoisomerase II are incubated for 30 min at 37 ℃ and are stopped with 1% sodium dodecyl sulfate (SDS) and proteinase K (100 μg/mL). The percentages of decatenation and inhibition of topoisomerase II by Etoposide are obtained [5].
细胞实验 After the Etoposide treatment, cells are removed from the dish with phosphate-buffered saline (PBS) containing 0.03% trypsin and 0.27 mM ethylenediaminetetraacetic acid (EDTA) and are diluted into culture dishes in appropriate numbers to yield between 20 and 200 colonies. After 12 days, cultures are fixed with methanol-acetic acid, stained with crystal violet, and scored for colonies containing more than 50 cells [5].
动物实验 The in vivo model for nude mice HB (NMHB) has been established. Only HB cells with embryonal components are grafted and reproduced successfully in this model. Each NMHB subsequently is transplanted into 50 mice for treatment groups. Treatment is initiated when the majority of the tumors reach a volume of 50-100 mm3. The mice are stratified according to their tumor volume and randomly assigned to groups of ten animals each. The animals injected with tumor are given ifosfamide, cisplatin, doxorubicin, etoposide (10 mg/kg/day, i.v.), and carboplatin as single agents in two blocks. One group of ten animals for each original xenograft served as a control group. After initiation of treatment, the tumor growth is recorded at 5-day intervals for 25-30 days and the relative tumor volumes are calculated. Twenty-four hours before the animals are sacrificed, bromodeoxyuridine (BrdU) is injected intraperitoneally for the semiquantitative determination of proliferation activity of the tumor cells (50 μg of BrdU/g body weight) [4].
别名 VP-16, 依托泊苷, 依托泊甙, VP-16-213
分子量 588.56
分子式 C29H32O13
CAS No. 33419-42-0

存储

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

溶解度

DMSO: 58.9 mg/mL (100 mM)

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 1.6991 mL 8.4953 mL 16.9906 mL 42.4766 mL
5 mM 0.3398 mL 1.6991 mL 3.3981 mL 8.4953 mL
10 mM 0.1699 mL 0.8495 mL 1.6991 mL 4.2477 mL
20 mM 0.085 mL 0.4248 mL 0.8495 mL 2.1238 mL
50 mM 0.034 mL 0.1699 mL 0.3398 mL 0.8495 mL
100 mM 0.017 mL 0.085 mL 0.1699 mL 0.4248 mL

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参考文献

1. HGN ÇELEBİOĞLU, et al. Effects of thymoquinone and etoposide combination on cell viability and genotoxicity in human cervical cancer hela cells. Istanbul J Pharm. 2022; 52(3):258-264. 2. Litwiniec A, et al. Low-dose etoposide-treatment induces endoreplication and cell death accompanied by cytoskeletal alterations in A549 cells: Does the response involve senescence? The possible role of vimentin. Cancer Cell Int. 2013 Feb 5;13(1):9. 3. Jamil S, et al. Etoposide induces cell death via mitochondrial-dependent actions of p5Cancer Cell Int. 2015 Aug 7;15:79. 4. Suzuki M, et al. Anticancer activity of the combination of cisplatin and etoposide in endometrial cancer-bearing nude mice. Gynecol Oncol. 1991 Apr;41(1):41-5. 5. Panigrahy D, et al. Inhibition of tumor angiogenesis by oral etoposide. Exp Ther Med. 2010 Sep;1(5):739-746. 6. Lee KI, et al. Etoposide induces pancreatic β-cells cytotoxicity via the JNK/ERK/GSK-3 signaling-mediated mitochondria-dependent apoptosis pathway. Toxicol In Vitro. 2016 Jul 26. pii: S0887-2333(16)30147-3. 7. Calvani M, det al. Etoposide-Bevacizumab a new strategy against human melanoma cells expressing stem-like traits. Oncotarget. 2016 Jun 9. doi: 10.18632/oncotarget.9939. 8. Zhang J, Hirst A J, Duan F, et al. Darren Robinson, 3 Mark Jones, 2 Le Li, 4 Peizhe Wang, Peng Jiang, 4 Peter W. Andrews, 2 Ivana Barbaric, 2,* and Jie Na[J]. Anti-apoptotic Mutations Desensitize Human Pluripotent Stem Cells to Mitotic Stress and Enable Aneuploid Cell Survival. Stem Cell Reports. 9. Ruan C, Wang C, Gong X, et al. An integrative multi-omics approach uncovers the regulatory role of CDK7 and CDK4 in autophagy activation induced by silica nanoparticles[J]. Autophagy. 2020. 10. Weizhe Li, Hong-Yan Wang, Xiaolu Zhao, Hongguo Duan, Binghua Cheng, Yafei Liu, Mengjie Zhao et al. A methylation-phosphorylation switch determines Plk1 kinase activity and function in DNA damage repair [J]. Science Advances. 2019 Mar 6;5(3):eaau7566.

文献引用

1. Yang C, Xu H, Yang D, et al.A renal YY1-KIM1-DR5 axis regulates the progression of acute kidney injury.Nature Communications.2023, 14(1): 4261. 2. Qu Y Q, Song L L, Xu S W, et al.Pomiferin targets SERCA, mTOR, and P-gp to induce autophagic cell death in apoptosis-resistant cancer cells, and reverses the MDR phenotype in cisplatin-resistant tumors in vivo.Pharmacological Research.2023: 106769. 3. Wang D, Wang Y, Di X, et al.Cortical tension drug screen links mitotic spindle integrity to Rho pathway.Current Biology.2023 4. Ruan C, Wang C, Gong X, et al. An integrative multi-omics approach uncovers the regulatory role of CDK7 and CDK4 in autophagy activation induced by silica nanoparticles. Autophagy. 2020 5. Yang G, Wan P, Xiang Q, et al. E3 Ubiquitin Ligase ASB17 Promotes Apoptosis by Ubiquitylating and Degrading BCLW and MCL1. Biology-Basel. 2021, 10(3): 234. 6. Feng J, Xi Z, Jiang X, et al. Saikosaponin a enhances Docetaxel efficacy by selectively inducing death of dormant prostate cancer cells through excessive autophagy. Cancer Letters. 2022: 216011. 7. Li W, Wang H Y, Zhao X, et al. A methylation-phosphorylation switch determines Plk1 kinase activity and function in DNA damage repair. Science Advances. 2019, 5(3): eaau7566 8. Zhang J, Hirst A J, Duan F, et al. Darren Robinson, 3 Mark Jones, 2 Le Li, 4 Peizhe Wang, Peng Jiang, 4 Peter W. Andrews, 2 Ivana Barbaric, 2,* and Jie Na[J]. Anti-apoptotic Mutations Desensitize Human Pluripotent Stem Cells to Mitotic Stress and Enable Aneuploid Cell Survival. Stem Cell Reports. 2019, 12(3): 557-571 9. Kong Y, Liu Y, Li X, et al.Palmitoylation landscapes across human cancers reveal a role of palmitoylation in tumorigenesis.Journal of Translational Medicine.2023, 21(1): 1-19. 10. Wu X, Yi X, Zhao B, et al.The volume regulated anion channel VRAC regulates NLRP3 inflammasome by modulating itaconate efflux and mitochondria function.Pharmacological Research.2023: 107016.
Topotecan hydrochloride Camptothecin Lurtotecan Bisantrene Gatifloxacin Betulinic acid CH-0793076 Lauterine

相关化合物库

该产品包含在如下化合物库中:
抗癌活性化合物库 抗癌上市药物库 抗癌临床化合物库 苗药化合物库 抗癌药物库 微生物天然产物库 经典已知活性库 临床期小分子药物库 抗癌天然产物库 FDA上市及药典收录分子库

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体内实验配液计算器

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

Etoposide 33419-42-0 Apoptosis Autophagy DNA Damage/DNA Repair Microbiology/Virology Mitophagy Topoisomerase Antibacterial Antibiotic VP-16 P388 HCT116 p53 chemotherapy Mitochondrial Autophagy FBXW Inhibitor anti-cancer inhibit VP 16 Bacterial 依托泊苷 prodrug 依托泊甙 VP-16-213 VP16 leukemia inhibitor

 

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