Aclacinomycin A hydrochloride (Synonyms: Aclarubicin hydrochloride)

Cat. No.: HY-N2306A: FAQs
Data Sheet SDS COA Handling Instructions

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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.

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Aclacinomycin A hydrochloride Chemical Structure

CAS No. : 75443-99-1

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Other Forms of Aclacinomycin A hydrochloride:

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3 Publications Citing Use of MCE Aclacinomycin A hydrochloride

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•Related Small Molecules:

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Topoisomerase Topo I Topo II

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Aminoglycoside Glycopeptide Lipopeptide Macrolide Oxazolidinone Quinolone Tetracycline β-lactam

Biological Activity
Purity & Documentation
References
Customer Review

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].
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].

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

Cell Viability Assay^[2]

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 Proliferation Assay^[2]

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 (0.75-6 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].

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.

Clinical Trial

Molecular Weight

848.33

Formula

C₄₂H₅₄ClNO₁₅

CAS No.

75443-99-1

Appearance

Solid

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

Structure Classification

Initial Source

Microorganisms

Streptomyces galilaeus

Shipping

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)

Solvent & Solubility

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.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.1788 mL	5.8939 mL	11.7879 mL
5 mM	0.2358 mL	1.1788 mL	2.3576 mL
10 mM	0.1179 mL	0.5894 mL	1.1788 mL

View the 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.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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.

Protocol 1

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.
Protocol 2

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:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: 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)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

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.

Purity & Documentation

Purity: 95.16%

Select Batch:

Data Sheet (286 KB) SDS (252 KB)

COA (261 KB) RP-HPLC (228 KB)

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, 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

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

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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