Aclacinomycin AAclacinomycin A
MedChemExpress (MCE)
HY-N2306
57576-44-0
Aclarubicin
98.94%
4°C, protect from light *In solvent : -80°C, 6 months
-20°C, 1 month (protect from light)
Room temperature in continental US
may vary elsewhere.
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[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]. 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)[3].
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].
Topoisomerase I Topoisomerase II
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1117(2):131-5. [Content Brief]
[2]. 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]
[3]. 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]