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Aclacinomycin A
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Aclacinomycin A图片
CAS NO:57576-44-0
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品名称
Aclarubicin
产品介绍
Aclacinomycin A (Aclarubicin) 是一种口服有效的蒽环类抗肿瘤的抗生素 (antibiotic)。Aclacinomycin A 是拓扑异构酶 (topoisomerase) I 和 II 的抑制剂。Aclacinomycin A 可抑制核酸的合成,特别是RNA的合成。Aclacinomycin A 可能抑制 26S 蛋白酶复合体以及泛素-ATP 依赖性蛋白水解。
生物活性

Aclacinomycin A (Aclarubicin) is an orally active and potent anthracycline antitumorantibiotic. Aclacinomycin A is an inhibitor oftopoisomeraseIandII. Aclacinomycin A inhibits synthesis of nucleic acid, especiallyRNA. Aclacinomycin A might inhibit the 26S protease complex as well as the ubiquitin-ATP-dependent proteolysis[1][2][3].

IC50& Target

Topoisomerase I

 

Topoisomerase II

 

体外研究
(In Vitro)

Aclacinomycin A (0-120 μM, 30 min) inhibits the ubiquitin-ATP-dependent proteolytic activity of rabbit reticulocytes in a dose-dependent manner, with an IC50of 52 μM. But it does not inhibit the ubiquitination[1].
Aclacinomycin A inhibits ubiquitin-ATP-dependent proteolysis after the conjugation of ubiquitin to proteins[1].
Aclacinomycin A (0-2.4 μM, 3 h) inhibits the topo II catalytic activity[2].
Aclacinomycin A (0-1.8 μM, 3 h) has negative effect on the proliferative rate of V79 and irs-2 cells[2].
Aclacinomycin A emits fluorescence and that human-cervical cancer HeLa cells exposed to Aclacinomycin A exhibits bright fluorescence signals in the cytoplasm when fluorescence microscopy was performed using the red filter (excitation 530-550 nm/emission 575 nm)[3].

Cell Viability Assay[2]

Cell Line:V79 and irs-2 cells
Concentration:0, 0.006, 0.12, 1.2, and 2.4 μM
Incubation Time:3 h
Result:Inhibited the topo II catalytic activity in a dose-dependent manner. The loss of topo II catalytic activity in ACLA-treated cells was in all cases significant compared with non-treated cells.

Cell Proliferation Assay[2]

Cell Line:V79 and irs-2 cells
Concentration:0, 0.12, 0.25, 0.37, 0.6, 1.2, 1.8 μM
Incubation Time:3 h
Result:Showed a dose-dependent negative effect on the proliferative rate of V79 and irs-2 cells, but the reduction in surviving colonies was higher in the radiosensitive irs-2 cells for most of the ACLA doses tested.
体内研究
(In Vivo)

Aclacinomycin A (0.75-6 mg/kg, IP, daily) dose-dependently exhibits tumor growth in mice-based Leukemia P-388 model[4].
Aclacinomycin A (0.6-20 mg/kg, Orally, daily) exhibits an antitumor effect on leukemia L-1210[4].
Aclacinomycin A is very well absorbed in mice, rats, and dogs after its oral administration. The oral LD50(76.5 mg/kg) is about twice the iv LD50(35.6 mg/kg) in mice[4].

Animal Model:DBA/2, CDF1(BALB/c×DBA/2) mice with Leukemia P-388 (90-110 g)[4].
Dosage:0.75 mg/kg, 1.5 mg/kg, 3 mg/kg, 6 mg/kg
Administration:Intraperitoneal administration daily for 10 days starting 3 hr after transplantation.
Result:Inhibited tumor growth.
Animal Model:CDF1mouse with Leukemia L-1210[4]
Dosage:0.6 mg/kg, 1.25 mg/kg, 2.5 mg/kg, 5 mg/kg, 10 mg/kg, 20 mg/kg
Administration:Orally, daily for days 1-9
Result:Exhibited an antitumor effect on leukemia L-1210.
Clinical Trial
分子量

811.87

Formula

C42H53NO15

CAS 号

57576-44-0

结构分类
  • Quinones
  • Anthraquinones
来源

Streptomyces sp.

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.