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1mg |
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Amrubicin (SM-5887), a third-generation synthetic 9-amino-anthracycline, is a potent DNA topoisomerase II inhibitor with antineoplastic activity. It can be used for the research of cancer. Amrubicin intercalates into DNA and inhibits the activity of topoisomerase II, resulting in inhibition of DNA replication, and RNA and protein synthesis, followed by cell growth inhibition and cell death. This agent has demonstrated a higher level of anti-tumor activity than conventional anthracycline drugs without exhibiting any indication of the cumulative cardiac toxicity common to this class of compounds. It is marketed in Japan since 2002 by Sumitomo Pharmaceuticals.
ln Vitro |
Amrubicin (SM-5887) is a DNA topozyme II. Amrubicin (SM-5887) (2.5 μg/mL) enhances radiation response in human lung adenocarcinoma A549 cells [1]. Amrubicin inhibits LX-1, A549, A431 and BT-474 cell lines at IC50s of 1.1, 2.4, 0.61, and 3.0 μg/mL, respectively [2]. Amrubicin tuff U937 cells exhibit cell cycle features with an IC50 of 5.6 μM. Amrubicin (SM-5887) (20 μM) causes duct induction in U937 cells, activates caspase-3/7, and lowers mitochondrial membrane potential (Δψm) [3].
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ln Vivo |
Amrubicin (SM-5887) (25 mg/kg, intravenous injection) demonstrates strong anticancer effect against SCLC tumors Lu-24 and Lu-134; T/C values (which compare the treatment group's mean tumor growth rate to Article 14 of those tumors) were 17% and 9%, respectively, for those tumors on a daily basis. Amrubicin (SM-5887) (25 mg/kg, iv) in combination with ciprofloxacin and irinotecan effectively decreased tumor formation in mice with produced LX-1 cells, as compared to Amrubicin alone. In human cancer xenograft models, amrubicin (SM-5887) either by itself or in conjunction with Tegaf and Urinary End Base suppresses tumor growth [2].
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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.
[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. [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 |
Molecular Formula |
C₂₅H₂₅NO₉
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Molecular Weight |
483.47
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CAS # |
110267-81-7
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Related CAS # |
92395-36-3 (HCl);110267-81-7;110311-30-3;
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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; AMR; SM-5887; SM5887; SM 5887; Amirubicin Hydrochloride; Foreign brand name: Calsed
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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)
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Solubility (In Vitro) |
DMSO : ≥ 30 mg/mL (~62.05 mM)
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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 | 2.0684 mL | 10.3419 mL | 20.6838 mL | |
5 mM | 0.4137 mL | 2.0684 mL | 4.1368 mL | |
10 mM | 0.2068 mL | 1.0342 mL | 2.0684 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.