1. Cell Cycle/DNA Damage
  2. Topoisomerase DNA/RNA Synthesis
  3. Hydroxyrubicin

Hydroxyrubicin 是一种抗肿瘤剂。Hydroxyrubicin 可诱导拓扑异构酶 II (topoisomerase II) 介导的 DNA 断裂。Hydroxyrubicin 可诱导 DNA 解旋。Hydroxyrubicin 对肿瘤细胞具有显著的抑制作用。Hydroxyrubicin 可用于多药耐药 (MDR) 白血病的研究。

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Hydroxyrubicin

Hydroxyrubicin Chemical Structure

CAS No. : 73113-90-3

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生物活性

Hydroxyrubicin is an antitumor agent. Hydroxyrubicin can induce topoisomerase II-mediated DNA cleavage. Hydroxyrubicin induces DNA unwinding. Hydroxyrubicin has a significant inhibitory effect on tumor cells. Hydroxyrubicin can be used for the study of Multidrug-resistant (MDR) leukemia[1][2].

体外研究
(In Vitro)

Hydroxyrubicin (1-10 μM,30 分钟) 可诱导人 c-myc 起始 DNA 中拓扑异构酶 II 介导的 DNA 断裂[1]
Hydroxyrubicin (2.5-10 μM,30 分钟) 可诱导浓度依赖性的 DNA 解旋[1]
Hydroxyrubicin (1 小时) 在敏感的 KB3.1 细胞系中表现出比 Doxorubicin (HY-15142A) 略强的细胞毒性 (IC50:0.35 μM 和 0.8 μM),并且在 KB-V1 细胞中的细胞毒性是 Doxorubicin 的 20 倍 (IC50:2 μM 和 40 μM)[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

Hydroxyrubicin (25-79.1 mg/kg,静脉注射,单次注射/每周一次,持续 11 周) 通过去除 Doxorubicin (HY-15142A) 的 C-3' 氨基,显著降低小鼠的急性毒性和心脏毒性,同时在 P388/Dox 细胞异种移植小鼠模型中保持抗肿瘤活性[2]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Healthy ICR Swiss mice[2].
Dosage: 79.1 mg/kg
Administration: I.v., once
Result: Showed significant reduction in granulocytes.
Animal Model: Chronic cardiotoxicity was induced in healthy ICR Swiss mice through repeated administration[2].
Dosage: 12 mg/kg
Administration: I.v., once weekly for 11 weeks
Result: Mild lesions were observed in 5 out of 10 mice.
The degree of myocardial fibrosis was relatively mild.
Animal Model: The model was established using male BDF1 mice (weighing 18-22 g) by intraperitoneal injection of 1×106 P388/Dox leukemia cells (drug-resistant strain)[2].
Dosage: 25 mg/kg, 37.5 mg/kg, 50.0 mg/kg
Administration: I.v., once
Result: Showed activity in the range of 25-50 mg/kg and no toxicity or death.
分子量

544.50

Formula

C27H28O12

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Hydroxyrubicin
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HY-105510
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