Merck
所有图片(2)

E1383

Sigma-Aldrich

依托泊苷

synthetic, 95.0-105.0%, powder

别名:
VP-16-213, 4′-去甲基表鬼臼毒素 -(4,6-O-亚乙基-β-D-吡喃葡萄糖苷)
Empirical Formula (Hill Notation):
C29H32O13
CAS号:
分子量:
588.56
EC 号:
MDL编号:
PubChem化学物质编号:
NACRES:
NA.77

质量水平

200

生物来源

synthetic

测定

95.0-105.0%

形式

powder

颜色

white to off-white

pKa 

9.8

mp

236-251 °C (lit.)

抗生素抗菌谱

neoplastics

作用机制

DNA synthesis | interferes
enzyme | inhibits

创始人

Teva

SMILES string

COc1cc(cc(OC)c1O)[C@H]2[C@@H]3[C@H](COC3=O)[C@H](O[C@@H]4O[C@@H]5CO[C@@H](C)O[C@H]5[C@H](O)[C@H]4O)c6cc7OCOc7cc26

InChI

1S/C29H32O13/c1-11-36-9-20-27(40-11)24(31)25(32)29(41-20)42-26-14-7-17-16(38-10-39-17)6-13(14)21(22-15(26)8-37-28(22)33)12-4-18(34-2)23(30)19(5-12)35-3/h4-7,11,15,20-22,24-27,29-32H,8-10H2,1-3H3/t11-,15+,20-,21-,22+,24-,25-,26-,27-,29+/m1/s1

InChI key

VJJPUSNTGOMMGY-MRVIYFEKSA-N

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一般描述

依托泊苷由植物中所含的鬼臼毒素合成。

应用

依托泊苷用于:
  • 在二甲亚砜(DMSO)中制备药物储备溶液,分析比较 DT40 突变细胞的敏感性
  • 培养细胞进行细胞活力测定
  • 治疗neuro-2A细胞(脑神经瘤细胞),诱导细胞程序性死亡

生化/生理作用

依托泊苷用于治疗晚期睾丸癌、卡波西(Kaposi′s)肉瘤、非小细胞肺癌(NSCLC)、SCLC(小细胞肺癌)和淋巴瘤。
依托泊甙是一种抗肿瘤试剂,和拓扑异构酶II和DNA结合,增强DNA双链和单链剪切和可逆抑制解除。 在S期和G2期阻止细胞周期;诱导正常和肿瘤细胞系凋亡;抑制癌蛋白Mdm2的合成,引起Mdm2过量表达的肿瘤系细胞凋亡。

特点和优势

该化合物是由 Teva研发。想要浏览其他由制药公司开发的化合物以及已批准物/候选药物清单, 请单击此处
该化合物是ADME Tox和胞凋亡研究的特色产品。发现更多的ADME Tox细胞凋亡特色产品。想要了解有关生物活性小分子在其他研究领域应用的更多信息,请访问 sigma.com/discover-bsm

包装

无底玻璃瓶。内容物在插入式融锥内。

象形图

Exclamation markHealth hazard

警示用语:

Danger

危险分类

Acute Tox. 4 Oral - Carc. 1B - Repr. 2

储存分类代码

6.1C - Combustible, acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects

WGK

WGK 3

个人防护装备

Eyeshields, Gloves, type P1 (EN143) respirator filter, type P3 (EN 143) respirator cartridges

分析证书

请输入批号搜索分析证书(COA)。

原产地证书 (CofO)

请输入批号搜索原产地证书(COO)。

Product Information Sheet

更多文件

Quotes and Ordering

Differential and common DNA repair pathways for topoisomerase I-and II-targeted drugs in a genetic DT40 repair cell screen panel
Maede Y, et al.
Molecular Cancer Therapeutics, 13(1), 214-220 (2014)
Loss of TBL1XR1 disrupts glucocorticoid receptor recruitment to chromatin and results in glucocorticoid resistance in a B-lymphoblastic leukemia model
Jones CL, et al.
Test, jbc-M114 (2014)
Pharmacology and Therapeutics for Dentistry - E-Book, 700-700 (2010)
The latency-related gene of bovine herpesvirus 1 inhibits programmed cell death
Ciacci-Zanella J, et al.
Journal of Virology, 73(12), 9734-9740 (1999)
S K Mungamuri et al.
Oncogene, 34(19), 2461-2470 (2014-07-16)
Chromatin conformation has a major role in all cellular decisions. We showed previously that P53 pro-apoptotic target promoters are enriched with H3K9me3 mark and induction of P53 abrogates this repressive chromatin conformation by downregulating SUV39H1, the writer of this mark

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