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Aclarubicin (Aclacinon; Aclacin; Aclaplastin; Aclacinomycine; Jaclacin. ACM; Aclacinomycin A) is a natually occuring oligosaccharide and anthracycline anticancer antibiotic isolated from the bacterium Streptomyces galilaeus. Aclarubicin inhibits the synthesis of RNA and proteins as well as DNA replication and repair. It does this by intercalating into DNA and interacting with topoisomerases I and II.
| Targets |
Topoisomerase II; Topoisomerase I
|
|---|---|
| ln Vitro |
Aclacinomycin A (0-120 μM, 30 min) has an IC50 of 52 μM and suppresses rabbit reticulocytes' ubiquitin-ATP-dependent proteolytic activity in a dose-dependent reaction. On the other hand, it does not prevent ubiquitination [1].
Aclacinomycin A prevents ubiquitin-ATP-dependent proteolysis subsequent to ubiquitin's conjugation with proteins[1]. Aclacinomycin A (zero-2.4 μM, three hours) inhibits the catalytic activity of topo II [2]. Aclacinomycin A (0-1.8 μM, 3 h) inhibits the rate of V79 and irs-2 cell proliferation[2]. Aclacinomycin A emits fluorescence, and when fluorescence microscopy is carried out with the red filter (excitation 530-550 nm/emission 575 nm), human cervical cancer HeLa cells exposed to Aclacinomycin A show bright fluorescence signals in the cytoplasm[3]. |
| ln Vivo |
Aclacinomycin A (0.75-6 mg/kg, IP, daily) dose-dependently displays tumor growth in mice-based Leukemia P-388 model[4].
Aclacinomycin A (0.6-20 mg/kg, Orally, daily) shows an antitumor effect on leukemia L-1210[4]. Aclacinomycin A is highly well absorbed when given orally to mice, rats, and dogs. In mice, the oral LD50 (76.5 mg/kg) is approximately twice that of the IV LD50 (35.6 mg/kg)[4]. |
| Cell Assay |
ell 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. |
| Animal Protocol |
DBA/2, CDF1 (BALB/c×DBA/2) mice with Leukemia P-388 (90-110 g).
0.75 mg/kg, 1.5 mg/kg, 3 mg/kg, 6 mg/kg Intraperitoneal administration daily for 10 days starting 3 hr after transplantation. |
| References |
|
| Molecular Formula |
C42H53NO15
|
|---|---|
| Molecular Weight |
811.87
|
| Exact Mass |
811.34
|
| Elemental Analysis |
C, 62.14; H, 6.58; N, 1.73; O, 29.56
|
| CAS # |
57576-44-0
|
| Related CAS # |
57576-44-0; 75443-99-1 (HCl)
|
| Appearance |
Solid powder
|
| SMILES |
CC[C@]1(C[C@@H](C2=C(C3=C(C=C2[C@H]1C(=O)OC)C(=O)C4=C(C3=O)C(=CC=C4)O)O)O[C@H]5C[C@@H]([C@@H]([C@@H](O5)C)O[C@H]6C[C@@H]([C@@H]([C@@H](O6)C)O[C@H]7CCC(=O)[C@@H](O7)C)O)N(C)C)O
|
| InChi Key |
USZYSDMBJDPRIF-SVEJIMAYSA-N
|
| InChi Code |
InChI=1S/C42H53NO15/c1-8-42(51)17-28(33-22(35(42)41(50)52-7)14-23-34(38(33)49)37(48)32-21(36(23)47)10-9-11-26(32)45)56-30-15-24(43(5)6)39(19(3)54-30)58-31-16-27(46)40(20(4)55-31)57-29-13-12-25(44)18(2)53-29/h9-11,14,18-20,24,27-31,35,39-40,45-46,49,51H,8,12-13,15-17H2,1-7H3/t18-,19-,20-,24-,27-,28-,29-,30-,31-,35-,39+,40+,42+/m0/s1
|
| Chemical Name |
methyl (1R,2R,4S)-4-[(2R,4S,5S,6S)-4-(dimethylamino)-5-[(2S,4S,5S,6S)-4-hydroxy-6-methyl-5-[(2R,6S)-6-methyl-5-oxooxan-2-yl]oxyoxan-2-yl]oxy-6-methyloxan-2-yl]oxy-2-ethyl-2,5,7-trihydroxy-6,11-dioxo-3,4-dihydro-1H-tetracene-1-carboxylate
|
| Synonyms |
Aclacinon; Aclacin; Aclaplastin; Aclacinomycine Jaclacin; ACMA; clacinomycin A
|
| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
|---|
| Preparing Stock Solutions | 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 | |
| 10 mM | 0.1232 mL | 0.6159 mL | 1.2317 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT05264883 | Unknown | Drug: Venetoclax-Decitabine/ Azacitidine Association |
Acute Myeloid Leukemia | The First Affiliated Hospital with Nanjing Medical University |
March 1, 2021 | Phase 3 |
| NCT04254640 | Not yet recruiting | Drug: Aclarubicin Drug: G-CSF |
Elderly Patients Newly Diagnosed |
Sun Yat-sen University | March 1, 2021 | Phase 2 |
| NCT02723448 | Completed | Drug: aclarubicin | Vasculopathy, Retinal, With Cerebral Leukodystrophy Cerebroretinal Vasculopathy, Hereditary |
Washington University School of Medicine |
December 5, 2016 | Phase 1 |
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