| Bioactivity | 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]. |
| Invitro | Aclacinomycin A (0-120 μM，30 min) 以剂量依赖性方式抑制兔网织红细胞的泛素-ATP 依赖性蛋白水解活性，IC50 为 52 μM。但它不抑制泛素化[1]。 Aclacinomycin A 在泛素与蛋白质结合后抑制泛素-ATP 依赖的蛋白水解[1]。 Aclacinomycin A (0-2.4 μM，3 h) 抑制 topo II催化活性[2]。 Aclacinomycin A (0-1.8 μM，3 h) 对 V79 和 irs-2 细胞的增殖率 有负面影响 [2]。人宫颈癌 HeLa 细胞暴露于 Aclacinomycin A 时，细胞质中呈现明亮的荧光信号。可使用红色滤光片 (激发波长 530-550 nm/发射波长 575 nm) 进行显微镜检查[3]。 Cell Viability Assay[2] Cell Line: |
| In Vivo | Aclacinomycin A (0.75-6 mg/kg，IP，每日) 在基于小鼠的白血病 P-388 模型中以剂量依赖性方式表现出肿瘤生长[4]。 Aclacinomycin A (0.6 -20 mg/kg，Oralall，daily) 对白血病有抗肿瘤作用 L-1210[4]。 Aclacinomycin A 口服后在小鼠、大鼠和犬体内吸收良好。口服 LD50 (76.5 mg/kg) 约为小鼠静脉注射 LD50 (35.6 mg/kg) 的两倍[4]。 Animal Model: |
| Name | Aclacinomycin A hydrochloride |
| CAS | 75443-99-1 |
| Formula | C42H54ClNO15 |
| Molar Mass | 848.33 |
| Appearance | Solid |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | 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) |
| Reference | [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. [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. [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. [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. |
Aclacinomycin A hydrochloride
CAS: 75443-99-1 F: C42H54ClNO15 W: 848.33
Aclacinomycin A (Aclarubicin) hydrochloride is an orally active and potent anthracycline antitumor antibiotic. Aclacinom
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