产品
编 号:F394816
分子式:C42H53NO15
分子量:811.87
产品类型
结构图
CAS No: 57576-44-0
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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.
体内研究:
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.
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).