Aclacinomycin A

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

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。

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.

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).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.

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.Animal Model:DBA/2, CDF1 (BALB/c×DBA/2) mice with Leukemia P-388 (90-110 g).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 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.

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Cell Cycle/DNA Damage

Topoisomerase

Topoisomerase

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57576-44-0

811.87

C42H53NO15

>98% (HPLC)

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C(OC)(=O)[C@@H]1C2=C([C@@H](O[C@H]3C[C@H](N(C)C)[C@H](O[C@H]4C[C@H](O)[C@H](O[C@@H]5O[C@@H](C)C(=O)CC5)[C@H](C)O4)[C@H](C)O3)C[C@@]1(CC)O)C(O)=C6C(=C2)C(=O)C=7C(C6=O)=C(O)C=CC7

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(-20℃)

With Ice Pack

≥ 2 years