Aclacinomycin A
(Synonyms: 阿克拉霉素,Jaclacin,Aclarubicin,Aclarubicin A) 目录号 : GC10102
An anthracycline with antibiotic and anticancer activities
Cas No.:57576-44-0
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
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Aclacinomycin A is a dual inhibitor of topoisomerase I and II [1]. Aclacinomycin A is an anticancer drug which can reduce the tumor with minimal damage to normal cells. Aclacinomycin A shows potency against a wide variety of solid tumours and haematological malignancies. In A549, HepG2 and MCF-7 cells, Aclacinomycin A shows cytotoxic activity with IC50 values of 0.27μM, 0.32μM and 0.62μM, respectively. Aclacinomycin A induces cell apoptosis in these cells and the effects change to be necrosis when the incubation time is prolonged. Aclacinomycin A is demonstrated to increase the activity of both caspase-3 and caspase-8, thus inducing the activation of PARP. Apart from that, as an inhibitor of opoisomerases, Aclacinomycin A is found to induce DNA damage in V79 and irs-2 cells. Aclacinomycin A is used to treat acute leukaemias, lymphomas and other solid tumors through its inhibition of topo II [1, 2].
References:
[1] Hajji N, Mateos S, Pastor N, Domínguez I, Cortés F. Induction of genotoxic and cytotoxic damage by aclarubicin, a dual topoisomerase inhibitor. Mutat Res. 2005 May 2;583(1):26-35.[2] Rogalska A, Szwed M, Jó wiak Z. Aclarubicin-induced apoptosis and necrosis in cells derived from human solid tumours. Mutat Res. 2010 Jul 19;700(1-2):1-10.
| Cas No. | 57576-44-0 | SDF | |
| 别名 | 阿克拉霉素,Jaclacin,Aclarubicin,Aclarubicin A | ||
| Canonical SMILES | OC1=CC=CC(C(C2=C3C(O)=C4C([C@@H](C(OC)=O)[C@@](O)(CC)C[C@@H]4O[C@H]5C[C@H](N(C)C)[C@H](O[C@@H]6O[C@@H](C)[C@@H](O[C@@H]7O[C@@H](C)C(CC7)=O)[C@@H](O)C6)[C@H](C)O5)=C2)=O)=C1C3=O | ||
| 分子式 | C42H53NO15 | 分子量 | 811.87 |
| 溶解度 | Soluble in DMSO | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.2317 mL | 6.1586 mL | 12.3172 mL |
| 5 mM | 0.2463 mL | 1.2317 mL | 2.4634 mL |
| 10 mM | 0.1232 mL | 0.6159 mL | 1.2317 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Rethinking Biosynthesis of Aclacinomycin A
Molecules 2023 Mar 18;28(6):2761.36985733 PMC10054333
Aclacinomycin A (ACM-A) is an anthracycline antitumor agent widely used in clinical practice. The current industrial production of ACM-A relies primarily on chemical synthesis and microbial fermentation. However, chemical synthesis involves multiple reactions which give rise to high production costs and environmental pollution. Microbial fermentation is a sustainable strategy, yet the current fermentation yield is too low to satisfy market demand. Hence, strain improvement is highly desirable, and tremendous endeavors have been made to decipher biosynthesis pathways and modify key enzymes. In this review, we comprehensively describe the reported biosynthesis pathways, key enzymes, and, especially, catalytic mechanisms. In addition, we come up with strategies to uncover unknown enzymes and improve the activities of rate-limiting enzymes. Overall, this review aims to provide valuable insights for complete biosynthesis of ACM-A.
Aclacinomycin A
Cancer Treat Rev 1984 Dec;11(4):299-302.6598408 10.1016/0305-7372(84)90027-6
Current status of Japanese studies with the new anthracycline antibiotic Aclacinomycin A
Recent Results Cancer Res 1980;74:207-16.7003659 10.1007/978-3-642-81488-4_26
Fundamental and clinical studies on a new yellow anthracycline antibiotic Aclacinomycin A are reviewed. Favorable responses were seen in patients with acute leukemia refractory to daunomycin and adriamycin, malignant lymphoma, and breast, ovarian, lung, gastric, intestinal, and urinary bladder cancers by intravenous and intraperitoneal infusions or bladder instillation of Aclacinomycin A alone in the phase II study.
Aclacinomycin A: clinical development of a novel anthracycline antibiotic in the haematological cancers
Drugs Exp Clin Res 1986;12(1-3):275-82.3525076
Aclacinomycin A (aclarubicin; ACM) is a new class II anthracycline antibiotic. Preclinical studies suggested that ACM had approximately equivalent antitumour activity but produced substantially less cardiotoxicity compared to other anthracyclines. Because of the recognized importance of these compounds in the treatment of haematological tumours, clinical trials of ACM were initiated in the late 1970s. ACM has been extensively evaluated in patients with relapsed leukaemia and advanced malignant lymphoma. Analysis of results compiled from Europe, Japan, and the United States shows that ACM is probably equivalent to doxorubicin for remission induction of patients with relapsed acute non-lymphoblastic leukaemia. Initial studies using ACM alone and in combination with standard cytotoxic drugs in previously untreated patients compare favourably with the best standard treatment for this disease. The antitumour activity of ACM in patients with acute lymphoblastic leukaemia or malignant lymphoma who have previously received doxorubicin or daunorubicin is low, and the issue of whether ACM lacks clinical cross-resistance to other anthracyclines is unresolved. Acute cardiac arrhythmias have been observed following administration of ACM, but congestive cardiomyopathy has been uncommon. Results to date all indicate that ACM has fulfilled its early expectations of antileukaemic activity and reduced toxicity. These hypotheses should now be evaluated in prospective, randomized trials with conventional anthracyclines.
Aclacinomycin A in the treatment of experimental proliferative vitreoretinopathy. Efficacy and toxicity in the rabbit eye
Invest Ophthalmol Vis Sci 1993 Apr;34(5):1753-60.8473115
Purpose: Aclacinomycin A is an oligosaccharide anthracycline that, by contrast with daunomycin, lacks carcinogenicity. The authors evaluated the efficacy of Aclacinomycin A in prevention of experimental proliferative vitreoretinopathy (PVR) and its toxicity on the rabbit retina. Methods: Dutch-belted rabbit were used to create a model for traction retinal detachment. Seven to 10 days after vitreous gas compression, 25,000 homologous fibroblasts were injected into the vitreous cavity. Subsequently, the eyes received either sham injections or doses of 6, 30, or 60 nmol of Aclacinomycin A, respectively. The fundus findings were documented on days 7, 14, and 28 after the fibroblast injection. The toxicity studies were conducted according to the same protocol as was used for the efficacy evaluation but without the fibroblast injection. Simultaneous electroretinograms were recorded on days 0, 3, 7, and 14 from the right eyes that were injected with 30 or 60 nmol of Aclacinomycin A and the left eyes that were sham injected. Morphologic studies were conducted on the eyes enucleated on days 3, 7, and 14 after drug exposure. Results: Intraocular administration of 30 nmol of Aclacinomycin A on day 2 after fibroblast injection resulted in a detachment rate of 37.5% (controls, 100%; P < 0.01, by Fisher's exact test). Administration of 60 nmol of Aclacinomycin A 3 days after fibroblast injection resulted in a detachment rate of 26.7% (controls, 100%; P < 0.0001). Six nanomoles of Aclacinomycin A 3 days after fibroblast injection had no effect. No electroretinogram changes were present in eyes treated with 30 nmol of Aclacinomycin A. Such recordings from eyes exposed to 60 nmol of Aclacinomycin A demonstrated decreased a- and b-waves on day 3; these completely recovered by day 7. Morphologic studies of these eyes revealed no damage to the retina. Conclusions: These results suggest that Aclacinomycin A should be considered an alternative to daunomycin for treatment of human PVR because, in addition to its lack of carcinogenicity, it shows good efficacy and causes less retinal toxicity.