Aclacinomycin A

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^[1][2][3]. 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^[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].
1. Solution preparation^[3]
1.1 Preparation of stock solution
Solvent: DMSO
Concentration: 10 mM.
Storage: Store at -20°C or -80°C in dark after aliquoting. Avoid repeated freezing and thawing.
1.2 Preparation of working solution
Dilute to 1-10 µM with cell culture medium (optimized according to the experiment).
Note: The working solution should be prepared and used immediately. Keep it away from light.

2. Cell staining
2.1 HeLa cells are seeded in each well at a concentration of 2 × 10⁴ cells/80 μL.
2.2 Add 10 μM Aclacinomycin A.
2.3 For 30 min at 37°C in a CO2-free incubator.
2.4 The fluorescence intensity is measured with fluorescence microscopy (Ex/Em = 555/490-635 nm).
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].