| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
Purity: ≥98%
Aclarubicin HCl (Aclacinomycin A; Aclaplastin; Jaclacin), the hydrochloride salt of Aclarubicin, is a potent and natually occuring oligosaccharide anthracycline antineoplastic antibiotic extracted from the bacterium Streptomyces galilaeus. Aclarubicin intercalates into DNA and interacts with topoisomerases I and II, thereby inhibiting DNA replication and repair and RNA and protein synthesis. Aclarubicin is antagonistic to other agents that inhibit topoisomerase II, such as etoposide, teniposide and amsacrine. This agent is less cardiotoxic than doxorubicin and daunorubicin.
| ln Vitro |
At an IC50 of 52 μM, aclacinomycin A (0-120 μM, 30 min) quantitatively suppresses the rabbit reticulocyte red's ubiquitin-ATP-regulated protein activity. However, it does not prevent ubiquitination [1]. Topo II catalytic activity is inhibited by aclacinomycin A (0-2.4 μM, 3 h) [2]. V79 and irs-2 cell swelling rate is negatively impacted by aclacinomycin A (0-1.8 μM, 3 h) [2]. Bright fluorescent signals are seen in the cytoplasm of human cervical carcinoma HeLa cells upon exposure to aclarithromycin A. Use of a red filter is possible (excitation wavelength: 530-550 nm).
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|---|---|
| ln Vivo |
Aclacinomycin A is well absorbed postcervically in mice, stents, and dogs. Side wall LD50 (76.5 mg/kg) Cervical intravenous injection of LD50 (35.6 mg, daily) has an anti-tumor effect on leukemia L-1210 [4]. Akclarithromycin A (0.75-6 mg/kg, IP, daily) exhibits tumor growth in a dose-dependent manner in a mouse-based P-388 model of blood glucose [4].
|
| Cell Assay |
Cell Viability Assay[2]
Cell Types: V79 and irs-2 cells Tested Concentrations: 0, 0.006, 0.12, 1.2, and 2.4 μM Incubation Duration: 3 h Experimental Results: Inhibition ./emission wavelength 575 nm) for lung cancer screening [3]. Topo II catalytic activity was dose-dependent. In all cases, the loss of topo II catalytic activity in ACLA-treated cells was significant compared with untreated cells. Cell proliferation assay[2] Cell Types: V79 and irs-2 Cell Tested Concentrations: 0, 0.12, 0.25, 0.37, 0.6, 1.2, 1.8 μM Incubation Duration: 3 hrs (hours) Experimental Results: V79 shows a dose-dependent negative effect on proliferation rate and irs-2 cells, but the reduction in viable colonies was higher in radiosensitive irs-2 cells for most ACLA doses tested. |
| Animal Protocol |
Animal/Disease Models: Multiples of leukemia P-388 [4. /kg) [4].
Doses: 0.75 mg/kg, 1.5 mg/kg, 3 mg/kg, 6 mg/kg. Route of Administration: intraperitoneally (ip) (ip) administered daily starting 3 hrs (hrs (hours)) after transplantation for 10 days Experimental Results: Inhibition of tumor growth. Animal/Disease Models: CDF1 mice with leukemia L-1210[4] Doses: 0.6 mg/kg, 1.25 mg/kg, 2.5 mg/kg, 5 mg/kg, 10 mg/kg, 20 mg/kg Route of Administration: Orally administered, one time/day on days 1-9. Experimental Results: demonstrated anti-tumor effect on leukemia L-1210. |
| References |
|
| Additional Infomation |
Aclarubicin hydrochloride is an anthracycline.
An anthracycline produced by Streptomyces galilaeus. It has potent antineoplastic activity. |
| Molecular Formula |
C42H54CLNO15
|
|---|---|
| Molecular Weight |
848.328860000001
|
| Exact Mass |
847.318
|
| CAS # |
75443-99-1
|
| Related CAS # |
Aclacinomycin A;57576-44-0
|
| PubChem CID |
153751
|
| Appearance |
Light yellow to yellow solid powder
|
| Boiling Point |
897.7ºC at 760 mmHg
|
| Melting Point |
151-153℃
|
| Flash Point |
496.7ºC
|
| LogP |
3.959
|
| Hydrogen Bond Donor Count |
5
|
| Hydrogen Bond Acceptor Count |
16
|
| Rotatable Bond Count |
10
|
| Heavy Atom Count |
59
|
| Complexity |
1530
|
| Defined Atom Stereocenter Count |
13
|
| 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.Cl
|
| InChi Key |
KUSMIBXCRZTVML-ZRMZNYNWSA-N
|
| InChi Code |
InChI=1S/C42H53NO15.ClH/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,8,12-13,15-17H2,1-7H31H/t18-,19-,20-,24?,27-,28-,29-,30-,31-,35-,39+,40+,42+/m0./s1
|
| Chemical Name |
(1R,2R,4S)-methyl
4-(((2R,5S,6S)-4-(dimethylamino)-5-(((2S,4S,5S,6S)-4-hydroxy-6-methyl-5-(((2R,6S)-6-methyl-5-oxotetrahydro-2H-pyran-2-yl)oxy)tetrahydro-2H-pyran-2-yl)oxy)-6-methyltetrahydro-2H-pyran-2-yl)oxy)-2-ethyl-2,5,7-trihydroxy-6,11-dioxo-1,2,3,4,6,11-hexahydrotetracene-1-carboxylate
hydrochloride
|
| Synonyms |
Antibiotic MA144A1 ACMA. MA144A1Aclacin AclacinomycineAACM Aclacinomycinclacinon Aclaplastin Jaclacin Aclacinomycin A hydrochloride Aclarubicin
Hydrochloride
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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 Vitro) |
DMSO : ≥ 125 mg/mL (~147.35 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (2.45 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (2.45 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 |
*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 |
| NCT02723448 | COMPLETED | Drug: aclarubicin | Cerebroretinal Vasculopathy, Hereditary Vasculopathy, Retinal, With Cerebral Leukodystrophy |
Washington University School of Medicine | 2016-12-05 | Phase 1 |
| NCT05264883 | RECRUITING | Drug: Venetoclax-Decitabine/ Azacitidine-Aclarubicin Association Drug: Venetoclax-Decitabine/Azacitidine Association |
Acute Myeloid Leukemia | The First Affiliated Hospital with Nanjing Medical University |
2021-03-01 | Phase 3 |
| NCT03045627 | UNKNOWN STATUS | Drug: AraC Drug: Aclarubicin Drug: Peg-G-CSF Drug: G-CSF |
Acute Myeloid Leukemia | Shandong University | 2017-01 | Phase 2 |
| NCT04254640 | UNKNOWN STATUS | Drug: Cladribine Injection Drug: Aclarubicin Drug: G-CSF Drug: cytarabine |
Acute Myeloid Leukemia Elderly Patients Newly Diagnosed |
Sun Yat-sen University | 2021-03-01 | Phase 2 |
| NCT03181815 | UNKNOWN STATUS | Drug: Cladribine Drug: G-CSF Drug: Aclarubicin Drug: Cytarabine |
Acute Myeloid Leukemia Relapse Leukemia |
Sun Yat-sen University | 2016-01-01 | Phase 2 |
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