Aclacinomycin A hydrochloride
Based on 5 publication(s) in Google Scholar
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.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- CAS No.: 75443-99-1
- Formule: C42H54ClNO15
- Masse moléculaire:848.33
-
Stockage:
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)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Activité biologique
-
Chemical Information
-
Solvant et solubilité
- Pureté et documentation
- Références
-
Help & FAQs
-
HY-10227
BortezomibProteasome Inhibitor -
HY-18964
MG-101Cysteine Protease Inhibitor -
HY-100529
PD150606Calpain Inhibitor -
HY-10227R
Bortezomib (Standard)Proteasome Inhibitor -
HY-18741
VR23Trypsin-like/Chymotrypsin-like/Caspase-like proteasomes Inhibitor -
HY-P0018
PepstatinAspartic Protease Inhibitor -
HY-13259
MG-132Proteasome Inhibitor -
HY-13067
CelastrolAutophagy Inducer -
HY-10455
CarfilzomibProteasome Inhibitor -
HY-10453
IxazomibProteasome Inhibitor -
HY-18964G
MG-101 (GMP)Cysteine Protease Inhibitor -
HY-10452
Ixazomib citrateProteasome Inhibitor
Publications Citing Use of MedChemExpress (MCE) Aclacinomycin A hydrochloride
More
Customer Validation & Images
-
Cell Proliferation/Viability Assay
-
Bio/Physico-chemical Assay
Voir tous les produits spécifiques à Isoform Topoisomerase
MoreVoir tous les produits spécifiques à Isoform DNA/RNA Synthesis
MoreVoir tous les produits spécifiques à Isoform Antibiotic
More
Activité biologique
Description
IC50 & Target
|
Topoisomerase I |
Topoisomerase II |
In Vitro
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].
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. .
-
Cell Line:V79 and irs-2 cells
-
Concentration:0, 0.006, 0.12, 1.2, and 2.4 μM
-
Incubation Time:3 h
-
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.
-
Cell Line:V79 and irs-2 cells
-
Concentration:0, 0.12, 0.25, 0.37, 0.6, 1.2, 1.8 μM
-
Incubation Time:3 h
-
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.
In Vivo
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.
-
Animal Model:DBA/2, CDF1 (BALB/c×DBA/2) mice with Leukemia P-388[4.
-
Dosage:0.75 mg/kg, 1.5 mg/kg, 3 mg/kg, 6 mg/kg.
-
Administration:Intraperitoneal administration daily for 10 days starting 3 hr after transplantation.
-
Result:Inhibited tumor growth.
-
Animal Model:CDF1 mouse with Leukemia L-1210[4]
-
Dosage:0.6 mg/kg, 1.25 mg/kg, 2.5 mg/kg, 5 mg/kg, 10 mg/kg, 20 mg/kg
-
Administration:Orally, daily for days 1-9
-
Result:Exhibited an antitumor effect on leukemia L-1210.
Essai clinique
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
-
CAS No. 75443-99-1
-
Appearance Solid
-
Masse moléculaire 848.33
-
Formule C42H54ClNO15
-
Color Light yellow to yellow
-
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.Cl
-
Synonyms
Aclarubicin hydrochloride
-
Structure Classification
-
Initial Source
Streptomyces galilaeus
-
Livraison
Room temperature in continental US; may vary elsewhere.
-
Stockage
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)
Publications (5)
-
Journal Impact Factor
-
Most Recent
-
Biomolecules
Predictive and Prognostic Relevance of ABC Transporters for Resistance to Anthracycline Derivatives. [Abstract]2025 Jul 6;15(7):971. PMID: 40723843
Aclacinomycin A hydrochloride purchased from MedChemExpress. Usage Cited in: Biomolecules. 2025 Jul 6;15(7):971. [Abstract]
Aclacinomycin A (aclarubicin; 0-100 μM; 72 h) showed cytotoxicity for CCRF-CEM and multidrug-resistant P-glycoprotein overexpressing CEM-ADR5000 leukemia cells.
Aclacinomycin A hydrochloride purchased from MedChemExpress. Usage Cited in: Biomolecules. 2025 Jul 6;15(7):971. [Abstract]
Aclacinomycin A (aclarubicin; 5 μM; 0, 15, 30, 180 min) uptake did not differ significantly in CCRF-CEM and CEM/ADR5000 cells, indicating no impact of P-glycoprotein on its efflux inside the cells, confirming its low cross-resistance.
-
Int J Hyperthermia
Selecting ideal drugs for encapsulation in thermosensitive liposomes and other triggered nanoparticles. [Abstract]2022;39(1):998-1009. PMID: 35876089 -
-
-
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
Solvant et solubilité
In Vitro:
DMSO : ≥ 125 mg/mL (147.35 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (2.45 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (2.45 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureté et documentation
-
Fiche technique (287 KB)
-
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
-
Instruction de manipulation (2659 KB)
Références
[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]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.1788 mL | 5.8939 mL | 11.7879 mL | 29.4697 mL |
| 5 mM | 0.2358 mL | 1.1788 mL | 2.3576 mL | 5.8939 mL | |
| 10 mM | 0.1179 mL | 0.5894 mL | 1.1788 mL | 2.9470 mL | |
| 15 mM | 0.0786 mL | 0.3929 mL | 0.7859 mL | 1.9646 mL | |
| 20 mM | 0.0589 mL | 0.2947 mL | 0.5894 mL | 1.4735 mL | |
| 25 mM | 0.0472 mL | 0.2358 mL | 0.4715 mL | 1.1788 mL | |
| 30 mM | 0.0393 mL | 0.1965 mL | 0.3929 mL | 0.9823 mL | |
| 40 mM | 0.0295 mL | 0.1473 mL | 0.2947 mL | 0.7367 mL | |
| 50 mM | 0.0236 mL | 0.1179 mL | 0.2358 mL | 0.5894 mL | |
| 60 mM | 0.0196 mL | 0.0982 mL | 0.1965 mL | 0.4912 mL | |
| 80 mM | 0.0147 mL | 0.0737 mL | 0.1473 mL | 0.3684 mL | |
| 100 mM | 0.0118 mL | 0.0589 mL | 0.1179 mL | 0.2947 mL |
Aclacinomycin A hydrochloride Related Classifications
HY-N2306A Related Classifications
Powered by Bioz