Doxorubicin (Adriamycin) HCl (Synonyms: DOX) |
| Catalog No.GC17567 |
Le chlorhydrate de doxorubicine (hydroxydaunorubicine), un antibiotique anthracycline cytotoxique, est un agent chimiothérapeutique anti-cancer.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 25316-40-9
Sample solution is provided at 25 µL, 10mM.
Doxorubicin is a semi-synthesized anticancer agent derived from bacterial culture. [1] It is an anthracycline antibiotic. It is been widely used in blood cancers, solid tumors and sarcomas.
Doxorubicin intercalates into DNA double strand and inhibits the progression of DNA topoisomerase II, stopping replication process. [2] Doxorubicin also induces histone eviction from open chromatin, causing DNA damage and epigenetic deregulation. [3]
Doxorubicin is administrated intravenously. Approximately 75% of doxorubicin and its metabolites bind to plasma protein. Doxorubicin does not cross blood brain barrier. 50% of the drug is eliminated unchanged from the body mainly though bile excretion. The remaining undergoes one-electron reduction, two-electron reduction, and deglycosidation. The major metabolite is a potent membrane ion pump inhibitor, which is associated with cardiomyopathy. [4]
References:
[1]Brayfield, A, ed. (2013). Doxorubicin. Martindale: The Complete Drug Reference. Pharmaceutical Press. Retrieved 15 April 2014.
[2]Pommier Y., et al. (2010). DNA topoisomerases and their poisoning by anticancer and antibacterial drugs. Chemistry & Biology 17 (5): 421–433.
[3]Pang, B., et al. (2013). Drug-induced histone eviction from open chromatin contributes to the chemotherapeutic effects of doxorubicin. Nature Communications 4 (5): 1908
[4]Boucek RJ., et al. (1987). The major metabolite of doxorubicin is a potent inhibitor of membrane-associated ion pumps. A correlative study of cardiac muscle with isolated membrane fractions. J of Biol Chem 262: 15851-15856.
| Cell experiment: [1] | |
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Cell lines |
H9c2 cells |
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Preparation method |
The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while.Stock solution can be stored below -20°C for several months. |
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Reaction Conditions |
1 μg/ml, 2 hours |
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Applications |
H9c2 cells were treated with increased concentrations of Doxorubicin (0.1, 0.3, 0.5, and 1.0 μg/ml, equal to 0.17, 0.52, 0.85, and 1.71 μM separately) for 2 h, or treated with 0.3 μg/ml (equal to 0.52 μM) of Doxorubicin for the different time points. Doxorubicin induces strong AMPKα (Thr 172) and its downstream Acetyl-CoA carboxylase (ACC, Ser 79) phosphorylation in both time- and dose-dependent manner. AMPKα phosphorylation became obvious after 1 h of Doxorubicin treatment which was further sustained for at least 6 h. LKB1, the possible upstream kinase for AMPK, was also activated by Doxorubicin in H9c2 cells. |
| Animal experiment: [2] | |
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Animal models |
C57BL/10 mice |
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Dosage form |
Intraperitoneal injection, 20 mg/kg |
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Applications |
Five days after doxorubicin injection, mice displayed significantly impaired systolic (LVP, -29%; dP/dtmax, -45%), diastolic (dP/dtmin, -44%; stiffness, +275%), and global (SV, -61%; HR, -18%; CO,-68%) left ventricular (LV) function when compared with the placebo group. Both cardiac lipid peroxidation activity (+37%) and cardiac nitrotyrosine protein expression (+204%) were increased when compared with placebo mice. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: [1] Chen M B, Wu X Y, Gu J H, et al. Activation of AMP-activated protein kinase contributes to doxorubicin-induced cell death and apoptosis in cultured myocardial H9c2 cells. Cell biochemistry and biophysics, 2011, 60(3): 311-322. [2] Riad A, Bien S, Westermann D, et al. Pretreatment with statin attenuates the cardiotoxicity of Doxorubicin in mice. Cancer research, 2009, 69(2): 695-699. |
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| Cas No. | 25316-40-9 | SDF | |
| Synonymes | DOX | ||
| Chemical Name | (7S,9S)-7-[(2R,4S,5S,6S)-4-amino-5-hydroxy-6-methyloxan-2-yl]oxy-6,9,11-trihydroxy-9-(2-hydroxyacetyl)-4-methoxy-8,10-dihydro-7H-tetracene-5,12-dione;hydrochloride | ||
| Canonical SMILES | CC1C(C(CC(O1)OC2CC(CC3=C(C4=C(C(=C23)O)C(=O)C5=C(C4=O)C=CC=C5OC)O)(C(=O)CO)O)N)O.Cl | ||
| Formula | C27H29NO11.HCl | M.Wt | 579.98 |
| Solubility | 33.3mg/ml in Water(Need ultrasonic);DMSO : >20 mg/mL (34.48 mM; Need ultrasonic) | Storage | 4°C, protect from light |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.7242 mL | 8.621 mL | 17.242 mL |
| 5 mM | 0.3448 mL | 1.7242 mL | 3.4484 mL |
| 10 mM | 0.1724 mL | 0.8621 mL | 1.7242 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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Related Biological Data
QSG protected mice against DOX-induced cardiac injury and body weight loss. (B-C) The serum CK-MB and LDH concentrations (n=6).
After being seeded into96-well plates for 24 hours at a density of 6×104 cells/mL, the cells were then subjected to various DOX(GLPBIO) doses (0.1~2 μmol/L).
Journal of Ethnopharmacology, 2023: 117134. PMID: 37714227 IF: 5.3999 -
Related Biological Data
Inhibition of autophagy increased upregulated S100P-enhanced chemosensitivity. C. Inhibition of autophagy increased upregulated S100P-enhanced chemosensitivity.
Cells were subsequently treated for 24 h with ADM (0.2 μg/ml)(GLPBIO) or 48 h with Ara-C (4 μM), then cell viability was assayed using a CCK-8 kit.
Am J Cancer Res 14.3 (2024): 1121. PMID: 36385800 IF: 5.2999 -
Related Biological Data
Res alleviates Dox-induced cytotoxicity by inhibiting ferroptosis in H9C2 cells. (B) The viability of H9C2 cells in each group (n = 3).
H9C2 cells were treated with 1 μM Dox (GLPBIO, USA, dissolved in DMSO) for 24 h to establish the DIC model and 0.5 μM RSL3 for 6 h to establish the ferroptotic model.
Toxicol Appl Pharm (2023): 116794. PMID: 38142782 IF: 3.8001
Average Rating: 5 (Based on Reviews and 23 reference(s) in Google Scholar.)
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