Etoposide

製品コードS1225 バッチS122511

印刷

化学情報

Chemical Structure Synonyms VP-16213,VP-16 Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C29H32O13
分子量 588.56 CAS No. 33419-42-0
Solubility (25°C)* 体外 DMSO 100 mg/mL (169.9 mM)
Water Insoluble
Ethanol Insoluble
体内 （毎回新しく調製した物を用意してください）
Clear solution
5% DMSO 40% PEG 300 5% Tween 80 ddH2O
5.0mg/ml Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL PEG300, mix evenly to clarify it; add 50 μL Tween-80 to the above system, mix evenly to clarify it; then continue to add 500 μL ddH2O Dilute to 1 mL. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 Etoposide is a semisynthetic derivative of podophyllotoxin, which inhibits DNA synthesis via topoisomerase II inhibition activity which enhances double-strand and single-strand cleavage of DNA and reversibly inhibits repair by topoisomerase II binding. Etoposide induces autophagy, mitophagy and apoptosis.
in vitro

Etoposide inhibits DNA synthesis by forming a complex with topoisomerase II and DNA, which induces breaks in double stranded DNA and prevents repair by topoisomerase II binding. Accumulated breaks in DNA prevent entry into the mitotic phase of cell division, and lead to cell death. Etoposide acts primarily in the G2 and S phases of the cell cycle. [1] Etoposide inhibits the growth of murine angiosarcoma cell line (ISOS-1) in a 5 days-period with IC50 of 0.25 μg/mL. Cell growth of normal murine microvascular endothelial cells (mECs) is less sensitive to Etoposide with IC50 of 10 μg/mL). [2] Etoposide treated for 6 hr inhibits colonies of tetraploid variant of the human leukemic lymphoblast line CCRF-CEM with IC50 of 0.6 μM. [3] Etoposide treated for 2 hr inhibits growth of human pancreatic cancer cell line Y1, Y3, Y5, Y19, YM. YS, and YT with IC50s of 300 μg/mL, 300 μg/mL, 300 μg/mL, 91 μg/mL, 0.68 μg/mL, 300 μg/mL, 300 μg/mL, and 260 μg/mL, respectively. [4] Etoposide exposed for 1 hr inhibits growth of human glioma cell lines CL5, G142, G152, G111, and G5 with IC50 of 8, 9, 9.8, 10, and 15.8 μg/mL respectively for 12 days. Under same condition, the IC90 value is attained in cell lines CL5, G152, G142, and G111 at 26, 27, 32, and 33 μg/mL. Etoposide inhibition of topoisomerase II is homogeneous for each cell. The average inhibition rates are 15%, 21.8%, 31.8%, 41.5%, and 49.5% for 1, 2, 4, 8, and 16 μg Etoposide, respectively. [5]
in vivo

Etoposide administrated as a single agent is found to been ineffective in many xenografts growth, such as Heterotransplanted Hepatoblastoma NMHB1, and NMHB 2, [6] human neuroblastoma xenograft, [7] and human gastrointestinal cancer xenograft, [8] while the dose of 10 mg/kg i.p. Etoposide inhibits murine angiosarcoma cell ISOS-1 tumors in 36% of controls. [2] Etoposide induces tumor immunity in Lewis lung cancer. A single administration of 50 mg/kg Etoposide i.p., induces a 60% survival of C57B1/6 mice injected with Lewis lung cancer cell (3LL) over 60 days. About 40% of these surviving mice reject a subsequent challenge with 3LL, while none of control mice survive beyond 30 days. 3LL cells which have survived an 90% lethal concentration of Etoposide in vitro kill 75% of recipient mice, but 60% surviving mice reject challenge with 3LL. Splenocytes harvested from tumor rejecting mice protect naive mice injected with 3LL. [9]

プロトコル(参考用のみ)

キナーゼアッセイ 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.
細胞アッセイ 細胞株 Human glioma cell lines CL5
濃度 80 μg/mL
反応時間 1 hour
実験の流れ

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.
動物実験 動物モデル Murine angiosarcoma xenografts ISOS-1
投薬量 10 mg/kg
投与方法 i.p. every day for 5 days from day 7

カスタマーフィードバック

Data from [Data independently produced by BMC Cancer, 2014, 14, 483]

Data from [Data independently produced by , , Leukemia, 2015, 29: 1702–1712]

Data from [Data independently produced by , , Nature, 2018, 563(7729):131-136]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Synergistic antitumor activity between HER2 antibody-drug conjugate and chemotherapy for treating advanced colorectal cancer [ Cell Death Dis, 2024, 15(3):187] PubMed: 38443386
DNA damage-induced PARP/ALC1 activation leads to Epithelial-to-Mesenchymal transition stimulating homologous recombination. [ bioRxiv, 2024, 10.1101/2024.01.16.575847] PubMed: none
An African-Specific Variant of TP53 Reveals PADI4 as a Regulator of p53-Mediated Tumor Suppression [ Cancer Discov, 2023, 13(7):1696-1719] PubMed: 37140445
SRCAP mutations drive clonal hematopoiesis through epigenetic and DNA repair dysregulation [ Cell Stem Cell, 2023, 10.1016/j.stem.2023.09.011] PubMed: 37863054
Oncolytic Parapoxvirus induces Gasdermin E-mediated pyroptosis and activates antitumor immunity [ Nat Commun, 2023, 14(1):224] PubMed: 36641456
K6-linked ubiquitylation marks formaldehyde-induced RNA-protein crosslinks for resolution [ Mol Cell, 2023, 10.1016/j.molcel.2023.10.011] PubMed: 37951215
An inducible long noncoding RNA, LncZFHX2, facilitates DNA repair to mediate osteoarthritis pathology [ Redox Biol, 2023, 66:102858] PubMed: 37633048
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ATR-binding lncRNA ScaRNA2 promotes cancer resistance through facilitating efficient DNA end resection during homologous recombination repair [ J Exp Clin Cancer Res, 2023, 42(1):256] PubMed: 37775817
Patient- and xenograft-derived organoids recapitulate pediatric brain tumor features and patient treatments [ EMBO Mol Med, 2023, 15(12):e18199] PubMed: 38037472

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人間や獣医の診断であるか治療的な使用のためにでない。

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