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

Aclacinomycin A  (Synonyms: Aclarubicin)

Cat. No.: HY-N2306 Purity: 98.94%
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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.

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

Aclacinomycin A Chemical Structure

Aclacinomycin A Chemical Structure

CAS No. : 57576-44-0

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5 mg USD 480 In-stock
10 mg USD 850 In-stock
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Customer Review

Based on 3 publication(s) in Google Scholar

Other Forms of Aclacinomycin A:

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  • Biological Activity

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Description

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[1][2][3].

IC50 & Target

Topoisomerase I

 

Topoisomerase II

 

Cellular Effect
Cell Line Type Value Description References
DU-145 IC50
0.129 μM
Compound: 12
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
[PMID: 33064004]
HCT-116 IC50
0.04 μM
Compound: 12
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
[PMID: 33064004]
K562 IC50
0.076 μM
Compound: 12
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
[PMID: 33064004]
MEL-JUSO IC50
0.048 μM
Compound: 12
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
[PMID: 33064004]
PC-3 IC50
0.101 μM
Compound: 12
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
[PMID: 33064004]
U-87MG ATCC IC50
0.137 μM
Compound: 12
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
[PMID: 33064004]
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 (90-110 g)[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

811.87

Formula

C42H53NO15

CAS No.
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

Initial Source

Streptomyces sp.

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 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
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 (protect from 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)

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

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

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g

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(per animal)

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 99.30%

References

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 (protect from 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 1.2317 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
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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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Aclacinomycin A
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