盐酸阿霉素, DNA 拓扑异构酶 II alpha 抑制剂

Name: 盐酸阿霉素, DNA 拓扑异构酶 II alpha 抑制剂
SKU: D409016
Availability: InStock

CAS: 25316-40-9 货号: D409016 分子式: C₂₇H₂₉NO₁₁·HCl 分子量: 579.98 Beilstein号: 4229251 EC号: 246-818-3

854篇引用文献 COA

有货

级别和纯度: 10mM in DMSO

储存条件

-80℃储存

运输条件

特低温运输

规格

库存

价格

数量

1ml

D409016-1ml

现货

¥299.90

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概述规格名称和识别符技术文档高级数据关联靶点（人）质检证书（CoA,COO,BSE/TSE 和分析图谱) 化学和物理性质安全和危险性（GHS）此产品的引用文献技术文档和文章溶液计算器

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为什么选择此级别

，适用于对基线干扰要求严格的色谱和分析工作流程。

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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。

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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。

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文献证明

在色谱分析、有机合成和交叉偶联反应领域已被 854 篇同行评审文献引用。

概述

Doxorubicin (Adriamycin)是一种抗生素类试剂，抑制DNA拓扑异构酶II，且诱导DNA损伤和凋亡。抗肿瘤抗生素，在心脏线粒体DNA方面有阿霉素的效果。反相转录酶和RNA聚合酶的抑制剂，免疫抑制剂；可插入DNA链中。临床上是癌症化疗剂、主要用于急、慢性白血病、恶性淋巴瘤。

Information

In vitro

Doxorubicin, an antibiotic anthracycline, is commonly considered to exert its anti-tumor activity at two fundamental levels, altering DNA and producing free radicals to trigger apoptosis of cancer cells through DNA damage. Doxorubicin can block the synthesis of DNA by intercalating into the DNA strand, and inhibits DNA topoisomerase II (TOP2). Doxorubicin is most effective when cells are rapidly proliferating and expressing high levels of TOP2. Additionally, Doxorubicin can trigger apoptosis by producing ceramide (which prompts apoptosis by activating p53 or other downstream pathways such as JNK), the degradation of Akt by serine threonine proteases, the mitochondrial release of cytochrome c, increased FasL (death receptor Fas/CD95 ligand) mRNA production, and a greater production of free radicals. Pre-treatment with GSNO (nitrosoglutathione) suppresses the resistance in the doxorubicin-resistant breast cancer cell line MCF7/Dx, accompanied by enhanced protein glutathionylation and accumulation of doxorubicin in the nucleus. Doxorubicin induced G2/M checkpoint arrest are attributed to elevated cyclin G2 (CycG2) expression and phospho-modification of proteins in the ataxia telangiectasia mutated (ATM) and ATM and Rad3-related (ATR) signaling pathways. Doxorubicin inhibits AMP-activated protein kinase (AMPK), resulting in SIRT1 dysfunction, p53 accumulation, and increased cell death in mouse embryonic fibroblasts (MEFs) and cardiomyocytes, which can be further sensitized by pre-inhibition of AMPK. Doxorubicin elicits a marked heat shock response, and that either inhibition or silencing of heat shock proteins enhance the Doxorubicin apoptotic effect in neuroblastoma cells. Nanomolar Doxorubicin treatment of neuroblastoma cells causes dose-dependent over-ubiquitination of a specific set of proteins in the absence of measurable inhibition of proteasome, and loss of activity of ubiquitinated enzymes such as lactate dehydrogenase and α-enolase, the protein ubiquination patterns of which is similar to those with proteasome inhibitor Bortezomib, indicating that Doxorubicin may also exert its effect by damaging proteins.

In vivo

In vivo, Doxorubicin in combination with adenoviral MnSOD (AdMnSOD) plus 1,3-bis(2-chloroethyl)-1-nitrosourea (BCNU) has the greatest effect in decreasing the volumes of MB231 tumors and prolonging survival of mice. Although its use is limited by the chronic and acute toxic side effects it produces, Doxorubicin is essential in treating breast and oesophageal carcinomas, solid tumours in childhood, osteosarcomas, Kaposi\'s sarcoma, soft tissue sarcomas, and Hodgkin and non-Hodgkin lymphomas.
Cell Data

cell lines：

Concentrations：

Incubation Time：

Powder Purity:≥98%

规格

英文别名

NSC 123127, DOX, Doxorubicin hydrochloride, Hydroxydaunorubicin HCl

规格或纯度

10mM in DMSO

英文名称

Doxorubicin (Adriamycin) HCl

生化机理

盐酸多柔比星（阿霉素，NSC 123127，DOX，Hydroxydaunorubicin）是一种抗生素，可抑制 DNA 拓扑异构酶 II，诱导 DNA 损伤、有丝分裂和肿瘤细胞凋亡。多柔比星可降低 AMPK 的基础磷酸化。多柔比星可用于艾滋病病毒感染者的同时治疗，但发现它有很高的 HBV 再激活风险。

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 alpha 抑制剂

名称和识别符

EC号

246-818-3

分子类型

小分子

Isomeric SMILES

C[C@H]1[C@H]([C@H](C[C@@H](O1)O[C@H]2C[C@@](CC3=C2C(=C4C(=C3O)C(=O)C5=C(C4=O)C(=CC=C5)OC)O)(C(=O)CO)O)N)O.Cl

关联CAS

23214-92-8

分子量

579.98

Beilstein号

4229251

Reaxy-Rn

25324888

Reaxys-RN link address

https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=25324888&ln=

技术文档

📋 安全数据表 (SDS)

全面的危险、操作、储存及法规合规文件。

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✅ 分析证书 (COA)

批次质量数据。输入批号以获取对应 COA。

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📊 产品数据表

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🔬 规格说明书

该级别的完整质量属性和验收标准。

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高级数据

关联靶点（人）

S100A4 Tchem 蛋白质S100-A4(Protein S100-A4) (0 活性数据)

点击查看靶蛋白信息： S100A4

活性类型	活性值-log(M)	作用机制	期刊	参考文献(PubMed IDs)

TOP2A Tclin DNA拓扑异构酶2-α(DNA topoisomerase 2-alpha) (0 活性数据)

点击查看靶蛋白信息： TOP2A

活性类型	活性值-log(M)	作用机制	期刊	参考文献(PubMed IDs)

化学和物理性质

溶解性

Solubility (25°C) In vitro DMSO: 46 mg/mL (201.69 mM); Ethanol: 6 mg/mL (26.3 mM); Water: Insoluble;

比旋光度

+240 to +270 deg(C=0.1,MeOH)

熔点

216°C

安全和危险性（GHS）

WGK Germany

RTECS

QI9295900

Merck Index

3439

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):

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