Etoposide

产品编号 T0132   CAS 33419-42-0
别名: VP-16-213, VP-16

Etoposide inhibits DNA synthesis by forming a complex with topoisomerase II and DNA (IC50: 60.3 μM).

Etoposide结构式
Etoposide , CAS 33419-42-0
规格 库存 价格/RMB 数量
100 mg 上海现货 450.00
200 mg 上海现货 750.00
500 mg 上海现货 1650.00
1 mL * 10 mM (in DMSO) 上海现货 450.00
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纯度 99.19%
纯度 99.94%
纯度 99.93%
生物活性
化学信息
存储 & 溶解度
配制溶液
产品描述 Etoposide inhibits DNA synthesis by forming a complex with topoisomerase II and DNA (IC50: 60.3 μM).
靶点活性 Topo II
体外活性 Etoposide inhibits proliferation of a variety of adenocarcinoma cells (IC50s: 0.005-12,200 µM) and HUVEC cells (IC50: 0.249 µM) [2]. Etoposide is capable of causing cytotoxicity on pancreatic β-cells by inducing apoptosis through the JNK/ERK-mediated GSK-3 downstream-triggered mitochondria-dependent signaling pathway in RIN-m5F cells [1].
体内活性 Etoposide (25 mg/kg) reduces tumor growth in a Ma human embryonal carcinoma mouse xenograft model [3]. Etoposide (10 mg/kg/day, i.v.) with ifosfamide and carboplatin, reduces the tumor volume in the hepatoblastoma cell injected NMRI nude mice [4].
激酶实验 Topoisomerase II activity assay: 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.
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. The standard errors are typically less than 15% of the mean value unless otherwise stated.(Only for Reference) Cell lines: Human glioma cell lines CL5
别名 VP-16-213 , VP-16
纯度 99.94%
分子量 588.56
分子式 C29H32O13
CAS No. 33419-42-0

存储

0-4℃ for short term (days to weeks), or -20℃ for long term (months).

溶解度

DMSO: 58.9 mg/mL (100 mM)

( < 1 mg/ml refers to the product slightly soluble or insoluble )

溶液 1

30% propylene glycol, 5% Tween 80, 65% D5W: 30 mg/mL

文献引用

参考文献
1. Chen GL, et al. Nonintercalative antitumor drugs interfere with the breakage-reunion reaction of mammalian DNA topoisomerase II. J Biol Chem. 1984 Nov 10;259(21):13560-6. 2. Drevs J, et al. Antiangiogenic potency of various chemotherapeutic drugs for metronomic chemotherapy. Anticancer Res. 2004 May-Jun;24(3a):1759-63. 3. Osieka R, et al. Enhancement of etoposide-induced cytotoxicity by cyclosporin A. Cancer Chemother Pharmacol. 1986;18(3):198-202. 4. Fuchs, J., et al. Comparative activity of cisplatin, ifosfamide, doxorubicin, carboplatin, and etoposide in heterotransplanted hepatoblastoma. Cancer, 1998. 83(11): p. 2400-7. 5. Beauchesne P, et al. Etoposide sensitivity of radioresistant human glioma cell lines. Cancer Chemother Pharmacol. 1998;41(2):93-7. 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.

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