Amrubicin
Amrubicin (SM-5887) is a DNA topoisomerase II inhibitor, used for the research of cancer.
For research use only. We do not sell to patients.
- CAS No.: 110267-81-7
- Formula: C25H25NO9
- Molecular Weight:483.47
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
All Topoisomerase Isoforms
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Biological Activity
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Topoisomerase II |
Amrubicin (SM-5887) is a DNA topoisomerase II inhibitor. Amrubicin (SM-5887) (2.5 μg/mL) shows radio-enhancement effects on human lung adenocarcinoma A549 cells[1]. Amrubicin supresses the LX-1, A549, A431, and BT-474 cell lines, with IC50s of 1.1 ± 0.2, 2.4 ± 0.8, 0.61 ± 0.10 and 3.0 ± 0.3 μg/mL, respectively[2]. Amrubicin inhibits the cell cycle profile of U937 cells with an IC50 of 5.6 μM. Amrubicin (SM-5887) (20 μM) also induces apoptosis in U937 cells, activates caspase-3/7 and reduces the mitochondrial membrane potential (Δψm)[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 110267-81-7
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Appearance Solid
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Molecular Weight 483.47
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Formula C25H25NO9
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Color Orange to red
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SMILES
CC([C@@](C1)(N)C[C@H](O[C@@H]2OC[C@@H](O)[C@@H](O)C2)C(C1=C3O)=C(O)C4=C3C(C5=CC=CC=C5C4=O)=O)=O
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Synonyms
SM-5887
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : ≥ 30 mg/mL (62.05 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Protocol
Aliquots of cells are plated into 96-well microplates. Following cell adherence (1 day), experimental medium either containing or not containing the agents is added to each well. Cells are treated with serial dilutions of each agent individually and with two agents simultaneously at a fixed ratio of doses. After 3 days of incubation with agents at 37°C in 5% CO2, the numbers of viable cells are examined using WST-1 or AlamarBlue. The IC50 value is defined as the concentration inhibiting cell growth by 50% compared with the controls. Multiple drug effects are analyzed by calculating CIs. At least three independent experiments are carried out in triplicate. CI values are calculated based on the conservative assumption of mutually nonexclusive drug interactions. CI values less than and greater than 1 indicate synergism and antagonism, respectively, whereas a value of 1 indicates addition[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Female athymic nude mice, BALB/c nu/nu are injected s.c. with tumor fragments in the flank. A few weeks after this inoculation, mice bearing a tumor approximately 100-300 mm3 in volume are randomLy allocated into different treatment groups and a control group, each of which consisted of six to eight mice. Tumor diameters are serially measured with calipers, and estimated tumor volumes are calculated by the formula: (smaller diameter)3 × (larger diameter)/2. The dosages of the agents tested are as follows: Amrubicin (SM-5887) (25 mg/kg, i.v.), doxorubicin (12.5 mg/kg, i.v.), cisplatin (10 mg/kg, i.v.), irinotecan (120 mg/kg, i.v.), gemcitabine (300 mg/kg per day, q7d, i.p.), vinorelbine (16 mg/kg, i.p.), trastuzumab (100 mg/kg per day, twice per week × 2 weeks, i.p.), tegafur/uracil (28 mg/kg per day, 5qd, p.o.), and gefitinib (150 mg/kg per day, 5qd, p.o.). In the combination experiments, amrubicin is given approximately 1 h before the other agent on day 0. The tumor growth rate is calculated with the formula: Vn/V0, where Vn is the estimated tumor volume at day n and V0 is the estimated tumor volume at the initiation of the treatment (day 0). The T/C (%) values are calculated by comparing the mean tumor growth rates of the treated group with those of the control group for each day that the tumors are measured. The systemic toxicities of the treatments are assessed in terms of changes in body weight during the experiments. These are calculated as (Wn − W0)/W0 × 100 where Wn is the body weight at day n and W0 is the body weight at the initiation of the treatment (day 0)[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (284 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Hayashi S, et al. Enhancement of radiosensitivity by topoisomerase II inhibitor, amrubicin and amrubicinol, in human lung adenocarcinoma A549 cells and kinetics of apoptosis and necrosis induction. Int J Mol Med. 2006 Nov;18(5):909-15. [Content Brief]
[2]. Hanada M, et al. Amrubicin, a novel 9-aminoanthracycline, enhances the antitumor activity of chemotherapeutic agents against human cancer cells in vitro and in vivo. Cancer Sci. 2007 Mar;98(3):447-54. [Content Brief]
[3]. Hanada M, et al. Amrubicin induces apoptosis in human tumor cells mediated by the activation of caspase-3/7 preceding a loss of mitochondrial membrane potential. Cancer Sci. 2006 Dec;97(12):1396-403. Epub 2006 Sep 21. [Content Brief]
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. 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 |
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| DMSO | 1 mM | 2.0684 mL | 10.3419 mL | 20.6838 mL | 51.7095 mL |
| 5 mM | 0.4137 mL | 2.0684 mL | 4.1368 mL | 10.3419 mL | |
| 10 mM | 0.2068 mL | 1.0342 mL | 2.0684 mL | 5.1710 mL | |
| 15 mM | 0.1379 mL | 0.6895 mL | 1.3789 mL | 3.4473 mL | |
| 20 mM | 0.1034 mL | 0.5171 mL | 1.0342 mL | 2.5855 mL | |
| 25 mM | 0.0827 mL | 0.4137 mL | 0.8274 mL | 2.0684 mL | |
| 30 mM | 0.0689 mL | 0.3447 mL | 0.6895 mL | 1.7237 mL | |
| 40 mM | 0.0517 mL | 0.2585 mL | 0.5171 mL | 1.2927 mL | |
| 50 mM | 0.0414 mL | 0.2068 mL | 0.4137 mL | 1.0342 mL | |
| 60 mM | 0.0345 mL | 0.1724 mL | 0.3447 mL | 0.8618 mL |