1. Cell Cycle/DNA Damage Metabolic Enzyme/Protease Anti-infection
  2. Topoisomerase DNA/RNA Synthesis Proteasome Antibiotic
  3. Aclacinomycin A hydrochloride

Aclacinomycin A hydrochloride  (Synonyms: Aclarubicin hydrochloride)

Cat. No.: HY-N2306A
COA Handling Instructions

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.

For research use only. We do not sell to patients.

Aclacinomycin A hydrochloride Chemical Structure

Aclacinomycin A hydrochloride Chemical Structure

CAS No. : 75443-99-1

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Description

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].

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].

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].

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.
Molecular Weight

848.33

Appearance

Solid

Formula

C42H54ClNO15

CAS No.
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

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)

*"≥" 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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 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

*All of the co-solvents are available by MCE.
Purity & Documentation
References
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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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Product Name:
Aclacinomycin A hydrochloride
Cat. No.:
HY-N2306A
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