Aclacinomycin A
Based on 5 publication(s) in Google Scholar
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.
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- Purity: 96.22%
- CAS No.: 57576-44-0
- 화학식: C42H53NO15
- 분자량:811.87
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Aclacinomycin A
MoreAll Topoisomerase Isoforms
MoreAll DNA/RNA Synthesis Isoforms
MoreAll Antibiotic Isoforms
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Biological Activity
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Topoisomerase I |
Topoisomerase II |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| DU-145 | IC50 |
0.129 μM
Compound: 12
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Cytotoxicity in human DU-145 cells assessed as reduction in cell viability incubated for 2 hrs by Cell-titer-blue assay
Cytotoxicity in human DU-145 cells assessed as reduction in cell viability incubated for 2 hrs by Cell-titer-blue assay
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[PMID: 33064004] |
| HCT-116 | IC50 |
0.04 μM
Compound: 12
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Cytotoxicity in human HCT-116 cells assessed as reduction in cell viability incubated for 2 hrs by Cell-titer-blue assay
Cytotoxicity in human HCT-116 cells assessed as reduction in cell viability incubated for 2 hrs by Cell-titer-blue assay
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[PMID: 33064004] |
| K562 | IC50 |
0.031 μM
Compound: 2
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Cytotoxicity against human K562 cells incubated for 2 hrs by cell titre blue viability assay
Cytotoxicity against human K562 cells incubated for 2 hrs by cell titre blue viability assay
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[PMID: 37561481] |
| K562 | IC50 |
0.076 μM
Compound: 12
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Cytotoxicity in human K562 cells assessed as reduction in cell viability incubated for 2 hrs by Cell-titer-blue assay
Cytotoxicity in human K562 cells assessed as reduction in cell viability incubated for 2 hrs by Cell-titer-blue assay
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[PMID: 33064004] |
| MEL-JUSO | IC50 |
0.048 μM
Compound: 12
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Cytotoxicity in human MEL-JUSO cells assessed as reduction in cell viability incubated for 2 hrs by Cell-titer-blue assay
Cytotoxicity in human MEL-JUSO cells assessed as reduction in cell viability incubated for 2 hrs by Cell-titer-blue assay
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[PMID: 33064004] |
| MEL-JUSO | IC50 |
0.099 μM
Compound: 2
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Cytotoxicity against human MEL-JUSO cells incubated for 2 hrs by cell titre blue viability assay
Cytotoxicity against human MEL-JUSO cells incubated for 2 hrs by cell titre blue viability assay
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[PMID: 37561481] |
| PC-3 | IC50 |
0.101 μM
Compound: 12
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Cytotoxicity in human PC-3 cells assessed as reduction in cell viability incubated for 2 hrs by Cell-titer-blue assay
Cytotoxicity in human PC-3 cells assessed as reduction in cell viability incubated for 2 hrs by Cell-titer-blue assay
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[PMID: 33064004] |
| U2OS | IC50 |
0.209 μM
Compound: 2
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Cytotoxicity against human U2OS cells incubated for 2 hrs by cell titre blue viability assay
Cytotoxicity against human U2OS cells incubated for 2 hrs by cell titre blue viability assay
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[PMID: 37561481] |
| U-87MG ATCC | IC50 |
0.137 μM
Compound: 12
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Cytotoxicity in human U87 cells assessed as reduction in cell viability incubated for 2 hrs by Cell-titer-blue assay
Cytotoxicity in human U87 cells assessed as reduction in cell viability incubated for 2 hrs by Cell-titer-blue assay
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[PMID: 33064004] |
| YOSHIDA | IC50 |
<0.02 μM
Compound: Aclacinomycin
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Concentration inhibiting [3H]TdR incorporation in Yoshida sarcoma tumor cells in vitro in rats
Concentration inhibiting [3H]TdR incorporation in Yoshida sarcoma tumor cells in vitro in rats
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[PMID: 1322986] |
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].
Guide (The following is our recommended protocol. This protocol is only a guide and should be modified according to your specific needs).
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).
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:V79 and irs-2 cells
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Concentration:0, 0.006, 0.12, 1.2, and 2.4 μM
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Incubation Time:3 h
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Result:Inhibited the topo II catalytic activity in a dose-dependent manner. The loss of topo II catalytic activity in ACLA-treated cells was in all cases significant compared with non-treated cells.
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Cell Line:V79 and irs-2 cells
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Concentration:0, 0.12, 0.25, 0.37, 0.6, 1.2, 1.8 μM
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Incubation Time:3 h
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Result:Showed a dose-dependent negative effect on the proliferative rate of V79 and irs-2 cells, but the reduction in surviving colonies was higher in the radiosensitive irs-2 cells for most of the ACLA doses tested.
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:DBA/2, CDF1 (BALB/c×DBA/2) mice with Leukemia P-388 (90-110 g)[4].
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Dosage:0.75 mg/kg, 1.5 mg/kg, 3 mg/kg, 6 mg/kg
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Administration:Intraperitoneal administration daily for 10 days starting 3 hr after transplantation.
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Result:Inhibited tumor growth.
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Animal Model:CDF1 mouse with Leukemia L-1210[4]
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Dosage:0.6 mg/kg, 1.25 mg/kg, 2.5 mg/kg, 5 mg/kg, 10 mg/kg, 20 mg/kg
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Administration:Orally, daily for days 1-9
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Result:Exhibited an antitumor effect on leukemia L-1210.
Chemical Information
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CAS No. 57576-44-0
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Appearance Solid
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분자량 811.87
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화학식 C42H53NO15
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Color Light yellow to yellow
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SMILES
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
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Synonyms
Aclarubicin
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Structure Classification
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Initial Source
Streptomyces sp.
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (5)
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Journal Impact Factor
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Most Recent
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Biomolecules
Predictive and Prognostic Relevance of ABC Transporters for Resistance to Anthracycline Derivatives. [Abstract]2025 Jul 6;15(7):971. PMID: 40723843 -
Int J Hyperthermia
Selecting ideal drugs for encapsulation in thermosensitive liposomes and other triggered nanoparticles. [Abstract]2022;39(1):998-1009. PMID: 35876089 -
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Bioengineered
DNA topoisomerase II alpha promotes the metastatic characteristics of glioma cells by transcriptionally activating β-catenin. [Abstract]2022 Feb;13(2):2207-2216. PMID: 35012441
용액&용해도
DMSO : 50 mg/mL (61.59 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
순도&문서
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Data Sheet (286 KB)
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SDS (420 KB)
- English - EN (420 KB)
- Français - FR (420 KB)
- Deutsch - DE (420 KB)
- Norwegian - NO (420 KB)
- Español - ES (420 KB)
- Swedish - SV (420 KB)
- Italian - IT (420 KB)
- Korean - KR (420 KB)
- Portuguese - PT (420 KB)
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Handling Instructions (2659 KB)
References
[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, 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]
Complete Stock Solution Preparation Table
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.2317 mL | 6.1586 mL | 12.3172 mL | 30.7931 mL |
| 5 mM | 0.2463 mL | 1.2317 mL | 2.4634 mL | 6.1586 mL | |
| 10 mM | 0.1232 mL | 0.6159 mL | 1.2317 mL | 3.0793 mL | |
| 15 mM | 0.0821 mL | 0.4106 mL | 0.8211 mL | 2.0529 mL | |
| 20 mM | 0.0616 mL | 0.3079 mL | 0.6159 mL | 1.5397 mL | |
| 25 mM | 0.0493 mL | 0.2463 mL | 0.4927 mL | 1.2317 mL | |
| 30 mM | 0.0411 mL | 0.2053 mL | 0.4106 mL | 1.0264 mL | |
| 40 mM | 0.0308 mL | 0.1540 mL | 0.3079 mL | 0.7698 mL | |
| 50 mM | 0.0246 mL | 0.1232 mL | 0.2463 mL | 0.6159 mL | |
| 60 mM | 0.0205 mL | 0.1026 mL | 0.2053 mL | 0.5132 mL |
Aclacinomycin A Related Classifications
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