计算溶液所需的质量、体积或浓度。
| 活性类型 | 活性值-log(M) | 作用机制 | 期刊 | 参考文献(PubMed IDs) |
|---|
有货
为什么选择此级别
Moligand™ 级 ，适用于对基线干扰要求严格的色谱和分析工作流程。
储存与运输
-80℃储存。特低温运输 。请查阅批次 COA 获取详细规格。
质量文档
SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。
文献证明
在色谱分析、有机合成和交叉偶联反应领域已被 12 篇同行评审文献引用。
概述
依托泊苷是一种抗肿瘤剂，它与拓扑异构酶Ⅱ及DNA结合成复合物，以增强双链和单链DNA的裂解，并可逆地抑制再连接。在细胞周期S期和G2期阻断细胞周期，在正常和肿瘤细胞系中诱导细胞凋亡，抑制癌蛋白Mdm2的合成，在过渡表达Mdm2的肿瘤细胞系中诱发细胞凋亡。Inhibits DNA synthesis via topoisomerase II inhibition
Etoposide (VP-16; VP-16-213) 是一种常用的抗肿瘤化疗剂。Etoposide 抑制拓扑异构酶 II (topoisomerase-II)，从而抑制 DNA 复制。Etoposide 诱导细胞周期停滞，凋亡 (apoptosis) 和自噬 (autophagy)。
Information
Etoposide (VP-16, VP-16213) is a semisynthetic derivative of podophyllotoxin, which inhibits DNA synthesis viatopoisomerase IIinhibition activity. Etoposide inducesautophagy,mitophagyandapoptosis.
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. 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). Etoposide treated for 6 hr inhibits colonies of tetraploid variant of the human leukemic lymphoblast line CCRF-CEM with IC50 of 0.6 μM. 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. 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.
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, human neuroblastoma xenograft, and human gastrointestinal cancer xenograft, while the dose of 10 mg/kg i.p. Etoposide inhibits murine angiosarcoma cell ISOS-1 tumors in 36% of controls. 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.
Cell Data
cell lines：
Concentrations：80 μg/mL
Incubation Time：1 hour
Powder Purity:≥99%
规格
英文别名
VP-16213 | Furo[3',4':6,7]naphtho[2,3-d]-1,3-dioxol-6(5aH)-one, 9-[(4,6-O-ethylidene-β-D-glucopyranosyl)oxy]-5,8,8a,9-tetrahydro-5-(4-hydroxy-3,5-dimethoxyphenyl)-, [5R-[5α,5aβ,8aα,9β(R*)]]-
规格或纯度
Moligand™, 10mM in DMSO
英文名称
Etoposide (VP-16)
生化机理
依托泊苷（VP-16，VP-16213）是荚膜多酚的半合成衍生物，通过抑制拓扑异构酶 II 的活性抑制 DNA 合成。依托泊苷能诱导自噬、有丝分裂和细胞凋亡。
储存条件
-80℃储存
运输条件
特低温运输
作用类型
抑制剂
作用机制
DNA 拓扑异构酶 II 抑制剂
名称和识别符
EC号
251-509-1
分子类型
小分子
Isomeric SMILES
C[C@@H]1OC[C@@H]2[C@@H](O1)[C@@H]([C@H]([C@@H](O2)O[C@H]3[C@H]4COC(=O)[C@@H]4[C@@H](C5=CC6=C(C=C35)OCO6)C7=CC(=C(C(=C7)OC)O)OC)O)O
关联CAS
分子量
588.56
Reaxy-Rn
365969
技术文档
高级数据
产品属性
| ALogP | 0.6 |
|---|
关联靶点（人）
TOP2B
Tclin
DNA拓扑异构酶2-β(DNA topoisomerase 2-beta)
(2 活性数据)
TOP2A
Tclin
DNA拓扑异构酶2-α(DNA topoisomerase 2-alpha)
(1 活性数据)
NCOA3
Tchem
核受体辅激活因子 3(Nuclear receptor coactivator 3)
(1 活性数据)
化学和物理性质
溶解性
Solubility (25°C) In vitro Ethanol: 15 mg/mL (64.91 mM); DMSO: 12 mg/mL (51.93 mM); Water: Insoluble;
比旋光度
-110.5° (C=0.6,CHCl3)
熔点
251°C
安全和危险性（GHS）
信号词
危险
危险声明
H302: 吞食有害
H350: 可能导致癌症
WGK Germany
3
RTECS
KC0190000
Merck Index
3886
个人防护装备
Eyeshields, full-face particle respirator type N100 (US), Gloves, respirator cartridge type N100 (US), type P1 (EN143) respirator filter, type P3 (EN 143) respirator cartridges
质检证书（CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:
技术文档和文章
ADME/Tox: From Basics to Advanced – Metabolizing Enzymes, Transporters and Key Tool Compounds
目录： 技术文章
Structural–Functional Analysis of the Methoxy Group (–OCH₃) in Approved Small-Molecule Drugs: Mechanisms, Evidence Chains, and Product-Selection Navigation (with Related Product Tables)
目录： 技术文章
The Key Starting Point for Phosphatidylserine Research: Changes in Membrane Localization, Functional Shifts, and Interpretation of Findings
目录： 技术文章
细胞周期与DNA损伤应答机制研究
目录： 技术文章
此产品的引用文献
溶液计算器
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