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Aclacinomycin A

CAS No. : 57576-44-0

MCE 站：Aclacinomycin A

产品活性：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。

研究领域：Cell Cycle/DNA Damage  |  Metabolic Enzyme/Protease  |  Anti-infection

作用靶点：Topoisomerase  |  DNA/RNA Synthesis  |  Proteasome  |  Antibiotic

结构分类：醌类  |  蒽醌类  |  结构分类

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 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).

In Vivo: Aclacinomycin A (0.75-6 mg/kg, IP, daily) dose-dependently exhibits tumor growth in mice-based Leukemia P-388 model.
Aclacinomycin A (0.6-20 mg/kg, Orally, daily) exhibits an antitumor effect on leukemia L-1210.
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.

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