Antibodies
Doxorubicin (Adriamycin)
- 貨號 Cat. No.
- S1208
- 規格 Size
- 5~200mg
- 品牌 Brand
- Selleckchem
Description
Doxorubicin (Adriamycin)Licensed by Pfizer
Doxorubicin (Adriamycin) is an antibiotic agent that inhibits DNA topoisomerase II and induces DNA damage and apoptosis.
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Distributor Tel: +886-2-2827-1197jimmy@new.abscience.com.tw
Biological Activity
| Description | Doxorubicin (Adriamycin) is an antibiotic agent that inhibits DNA topoisomerase II and induces DNA damage and apoptosis. | |||||
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| In vitro | Doxorubicin, an antibiotic anthracycline, is commonly considered to exert its anti-tumor activity at two fundamental levels, altering DNA and producing free radicals to trigger apoptosis of cancer cells through DNA damage. Doxorubicin can block the synthesis of DNA by intercalating into the DNA strand, and inhibits DNA topoisomerase II (TOP2). Doxorubicin is most effective when cells are rapidly proliferating and expressing high levels of TOP2. Additionally, Doxorubicin can trigger apoptosis by producing ceramide (which prompts apoptosis by activating p53 or other downstream pathways such as JNK), the degradation of Akt by serine threonine proteases, the mitochondrial release of cytochrome c, increased FasL (death receptor Fas/CD95 ligand) mRNA production, and a greater production of free radicals. [2] Pre-treatment with GSNO (nitrosoglutathione) suppresses the resistance in the doxorubicin-resistant breast cancer cell line MCF7/Dx, accompanied by enhanced protein glutathionylation and accumulation of doxorubicin in the nucleus. [3]Doxorubicin induced G2/M checkpoint arrest are attributed to elevated cyclin G2 (CycG2) expression and phospho-modification of proteins in the ataxia telangiectasia mutated (ATM) and ATM and Rad3-related (ATR) signaling pathways. [5] Doxorubicin inhibits AMP-activated protein kinase (AMPK), resulting in SIRT1 dysfunction, p53 accumulation, and increased cell death in mouse embryonic fibroblasts (MEFs) and cardiomyocytes, which can be further sensitized by pre-inhibition of AMPK. [6] Doxorubicin elicits a marked heat shock response, and that either inhibition or silencing of heat shock proteins enhance the Doxorubicin apoptotic effect in neuroblastoma cells. Nanomolar Doxorubicin treatment of neuroblastoma cells causes dose-dependent over-ubiquitination of a specific set of proteins in the absence of measurable inhibition of proteasome, and loss of activity of ubiquitinated enzymes such as lactate dehydrogenase and α-enolase, the protein ubiquination patterns of which is similar to those with proteasome inhibitor Bortezomib, indicating that Doxorubicin may also exert its effect by damaging proteins. [8] | |||||
| In vivo | In vivo, Doxorubicin in combination with adenoviral MnSOD (AdMnSOD) plus 1,3-bis(2-chloroethyl)-1-nitrosourea (BCNU) has the greatest effect in decreasing the volumes of MB231 tumors and prolonging survival of mice. [1] Although its use is limited by the chronic and acute toxic side effects it produces, Doxorubicin is essential in treating breast and oesophageal carcinomas, solid tumours in childhood, osteosarcomas, Kaposi’s sarcoma, soft tissue sarcomas, and Hodgkin and non-Hodgkin lymphomas. [2] | |||||
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Protocol(Only for Reference)
Animal Study: [1]
| Animal Models | Female athymic nude mice injected s.c. with MB231 cells |
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| Dosages | 3 mg/kg/day |
| Administration | Delivered intratumorly |
| Solubility | 30% PEG400/0.5% Tween80/5% propylene glycol 30 mg/mL |
References
Clinical Trial Information( data from http://clinicaltrials.gov)
| NCT Number | Recruitment | Conditions | Sponsor /Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT01913652 | Not yet recruiting | Dedifferentiated Liposarcoma | European Organisation for Research and Treatment of Cancer - EORTC|Sanofi | 2014-02 | Phase 2 |
| NCT01539174 | Not yet recruiting | Contiguous Stage II Adult Diffuse Large Cell Lymphoma|Noncontiguous Stage II Adult Diffuse Large Cell Lymphoma|Stage I Adult Diffuse Large Cell Lymphoma|Stage III Adult Diffuse Large Cell Lymphoma|Sta | Fox Chase Cancer Center|Genentech | 2014-03 | Phase 2 |
| NCT02018458 | Not yet recruiting | Breast Cancer | Baylor Research Institute | 2014-03 | Phase 1|Phase 2 |
| NCT01751893 | Not yet recruiting | Palmar-plantar Erythrodysesthesia (PPE) | Cyprus University of Technology | 2014-03 | |
| NCT01969578 | Not yet recruiting | Salivary Gland Cancer | European Organisation for Research and Treatment of Cancer - EORTC | 2014-03 | Phase 2 |
Chemical Information
Download Doxorubicin (Adriamycin) SDF
| Molecular Weight (MW) | 579.98 |
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| Formula | C27H29NO11.HCl |
| CAS No. | 25316-40-9 |
| Storage | 3 years -20℃Powder |
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| 6 months-80℃in DMSO | |
| Syonnyms | N/A |
| Solubility (25°C) * | In vitro | DMSO | 100 mg/mL (172 mM) |
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| Water | 20 mg/mL (34 mM) | ||
| Ethanol | <1 mg/mL (<1 mM) | ||
| In vivo | 30% PEG400/0.5% Tween80/5% propylene glycol | 30 mg/mL | |
| * <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. | |||
| Chemical Name | (8S,10S)-10-((2R,4S,5S,6S)-4-amino-5-hydroxy-6-methyl-tetrahydro-2H-pyran-2-yloxy)-6,8,11-trihydroxy-8-(2-hydroxyacetyl)-1-methoxy-7,8,9,10-tetrahydrotetracene-5,12-dione hydrochloride |
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Preparing Stock Solutions
| Stock Solution (1ml DMSO) | 1mM | 10mM | 20mM | 30mM |
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| Mass(mg) | 0.57998 | 5.7998 | 11.5996 | 17.3994 |
Customer Reviews (3)
 Click to enlarge | Rating | |
| Source | J Biomed Mater Res Part A 2012:00A:000–000.. Doxorubicin (Adriamycin) purchased from Selleck | |
| Method | Release experiment | |
| Cell Lines | N.A. | |
| Concentrations | 0.25mg/mL | |
| Incubation Time | 2-10 h | |
| Results | Doxorubicin was loaded by equilibrium partitioning in the following manner: a stock solution of doxorubicin was prepared in 2 wt % DMSO in 1 PBS (pH 7.4) at a concentration of 0.25 mg/mL. A 5 mg/mL concentration of crushed particles (75–150 um) of P(MAA-g-EG) or P(MAA-g-EG) containing PMMA nanoparticles to doxorubicin stock solution was allowed to stir slowly for 2 h. |
Product Citations (11)
SIRT1 and AMPK mediate hypoxia-induced resistance of non-small cell lung cancers to cisplatin and doxorubicin. [Shin DH, et al. Cancer Res 2013;74(1):298-308]
An integrated chemical biology approach identifies specific vulnerability of Ewing’s sarcoma to combined inhibition of Aurora kinases A and B. [Winter GE, et al. Mol Cancer Ther 2011;10(10):1846-56]
A Novel Use of Gentamicin in the ROS-Mediated Sensitization of NCI- H460 Lung Cancer Cells to Various Anticancer Agents [Cuccarese MF ACS Chem Biol 2013;8(12):2771-7]
