Aclacinomycin A hydrochloride  (Synonyms: Aclarubicin hydrochloride)

Aclacinomycin A (Aclarubicin) hydrochloride is an orally active and potent anthracycline antitumor antibiotic. Aclacinomycin A hydrochloride is an inhibitor of topoisomerase I and II. Aclacinomycin A hydrochloride inhibits synthesis of nucleic acid, especially RNA. Aclacinomycin A hydrochloride might inhibit the 26S protease complex as well as the ubiquitin-ATP-dependent proteolysis^[1][2][3].

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

848.33

Solid

C₄₂H₅₄ClNO₁₅

75443-99-1

O=C([C@@H]1C2=CC(C(C3=CC=CC(O)=C43)=O)=C(C4=O)C(O)=C2[C@@H](O[C@@](O[C@@H](C)[C@H]5O[C@@](O[C@@H](C)[C@H]6O[C@](CCC7=O)([H])O[C@H]7C)([H])C[C@@H]6O)([H])C[C@@H]5N(C)C)C[C@]1(O)CC)OC.Cl

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

• [1]. Isoe T, et al. Inhibition of different steps of the ubiquitin system by CDDP and aclarubicin. Biochim Biophys Acta. 1992 Sep 15;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, et al. Antitumor activity of new anthracycline antibiotics, aclacinomycin-A and its analogs, and their toxicity. Gan. 1977 Oct;68(5):685-90.  [Content Brief]