Aclacinomycin A Aclarubicin|cas:57576-44-0|西域试剂

Aclacinomycin A Aclarubicin

产品编号：Bellancom-N2306| CAS NO：57576-44-0| 分子式：C₄₂H₅₃NO₁₅| 分子量：811.87

阿克拉霉素A（Aclarubicin）是一种口服有效的蒽环类抗肿瘤抗生素。阿克拉霉素A是拓扑异构酶I和II的抑制剂。阿克拉霉素A抑制核酸，特别是RNA的合成。阿克拉霉素A可能抑制26S蛋白酶复合物以及泛素ATP依赖性蛋白水解。

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货号	价格	库存与货期
Bellancom-N2306	￥1950.00	杭州北京（现货）
Bellancom-N2306	￥4800.00	杭州北京（现货）
Bellancom-N2306	￥8500.00	杭州北京（现货）

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Aclacinomycin A 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 antitumor antibiotic. Aclacinomycin A is an inhibitor of topoisomerase I and II. Aclacinomycin A inhibits synthesis of nucleic acid, especially RNA. Aclacinomycin A might inhibit the 26S protease complex as well as the ubiquitin-ATP-dependent proteolysis.

体外研究

Aclacinomycin A (0-120 μM, 30 min) inhibits the ubiquitin-ATP-dependent proteolytic activity of rabbit reticulocytes in a dose-dependent manner, with an IC₅₀ of 52 μM. But it does not inhibit the ubiquitination.
Aclacinomycin A inhibits ubiquitin-ATP-dependent proteolysis after the conjugation of ubiquitin to proteins.
Aclacinomycin A (0-2.4 μM, 3 h) inhibits the topo II catalytic activity.
Aclacinomycin A (0-1.8 μM, 3 h) has negative effect on the proliferative rate of V79 and irs-2 cells.
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).

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

Cell Viability Assay

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

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].

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

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:	CDF₁ mouse 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.

体内研究

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

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:	CDF₁ mouse 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.

体内研究

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

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:	CDF₁ mouse 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.

性状

溶解性数据

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.

参考文献

. Isoe T, et al. Inhibition of different steps of the ubiquitin system by CDDP and aclarubicin. Biochim Biophys Acta. 1992 Sep 15;1117(2):131-5. [Content Brief]

. Hajji N, et al. Induction of genotoxic and cytotoxic damage by aclarubicin, a dual topoisomerase inhibitor. Mutat Res. 2005 May 2;583(1):26-35. [Content Brief]

. Iihoshi H, et al. Aclarubicin, an anthracycline anti-cancer drug, fluorescently contrasts mitochondria and reduces the oxygen consumption rate in living human cells. Toxicol Lett. 2017 Aug 5;277:109-114. [Content Brief]

[4]. Hori S, Shirai M, Hirano S, Oki T, Inui T, Tsukagoshi S, Ishizuka M, Takeuchi T, Umezawa H. Antitumor activity of new anthracycline antibiotics, aclacinomycin-A and its analogs, and their toxicity. Gan. 1977 Oct;68(5):685-90. [Content Brief]

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产品编号(Item Number)

批号(Lot Number)

危害码 (欧洲)	T
风险声明 (欧洲)	R25
安全声明 (欧洲)	S36/37/39-S45
危险品运输编码	3249
RTECS号	QI9279300
包装等级	II
危险类别	6.1(a)

Aclacinomycin A Aclarubicin

Aclacinomycin A Aclarubicin

化学品安全说明书(MSDS)

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