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Doxorubicin
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Doxorubicin图片
包装与价格:
包装价格(元)
10mM (in 1mL Water)电议
10mg电议
25mg电议
100mg电议

产品介绍
多柔比星 (Hydroxydaunorubicin) 是一种具有细胞毒性的蒽环类抗生素,是一种抗癌化疗药物。

Cell lines

Human lung carcinoma (A549) cell lines

Preparation Method

About 1×105A549 cells/well were plated into 12-well culture dishes and incubated for 24h. After 24h, doxorubicin, as well as conjugates of doxorubicin at a concentration equivalent to 2μg/ml of doxorubicin was added and incubated for time periods of 4 and 12h.

Reaction Conditions

2μg/ml

Applications

The uptake of the free doxorubicin and conjugates into the A549 cells increased with time. The fluorescent images of cells treated with free doxorubicin and polymannose(PM)-doxorubicin showed better uptake, while the sodium alginate(SA)-doxorubicin showed significantly lesser uptake after 4 and 12h exposure.

Animal models

BALB/c mice (5-6 weeks, female) and BALB/c athymic nude mice (nu/nu, 5-6 weeks, male)

Preparation Method

For in vivo tumor implantation, C26 cells at 5×105cells in 30μL Minimum Essential Medium (MEM) and MIA PaCa-2 cells at 2×106cells in 50μL 10:90 v/v MEM: Matrigel matrix were inoculated in the right flank of normal and athymic nude BALB/c mice, respectively. Tumor cells were allowed to grow until the tumor volume-reached 75-100mm3for C26 tumors and 100-125mm3 for MIA PaCa-2 tumors. Tumor-bearing mice were then treated with a single i.v. injection of albumin-binding domain-doxorubicin (ABD-DoX) at 10 and 20mg doxorubicin equiv. kg-1BW, AlDoxorubicin at 20mg doxorubicin equiv. kg-1BW, and free doxorubicin at 10mg·kg-1BW.

Dosage form

ABD-Doxorubicin at 10 and 20mg doxorubicin equiv. kg-1 BW, AlDoxorubicin at 20mg doxorubicin equiv. kg-1BW, and free doxorubicin at 10mg kg-1BW.

Applications

ABD-Doxorubicin has superior therapeutic efficacy to AlDoxorubicin in the syngeneic C26 colon carcinoma model in BALB/c mice and in the MIA PaCa-2 pancreatic adenocarcinoma xenograft model in nude mice, and that both formulations are superior to free Doxorubicin.

文献引用
产品描述

Doxorubicin(DOX), also known as adriamycin, is a compound of the anthracycline class that has the broadest spectrum of activity[1]. Doxorubicin inhibits topoisomerase Ⅱ and topoisomerase Ⅰ with IC50of 2.67μM and 0.8μM, respectively[2,3]. It is widely used for the treatment of various solid tumors via interacting with deoxyribonucleic acid, but it is limited in the clinical application due to severe side effect[4]

Doxorubicin can be loaded into liposomes by transmembrane pH gradient method to get high encapsulation efficiency with high drug/lipid ratio. Liposomal doxorubicin is a successful clinical formulation, and also a perfect model drug system for cancer-therapy research[5]. A considerable amount of doxorubicin can accumulate in human placental tissue. Both doxorubicin and its pH-sensitive liposomal formulation, L-Doxorubicin, are efficiently internalized by human trophoblastic BeWo cells and that doxorubicin accumulates in placental tissue so that decrease the exposure of fetal[6]

Doxorubicin combines with cobimetinib at sublethal dose completely arrested osteosarcoma growth. Targeted MEK inhibition by cobimetinib enhances doxorubicin’s efficacy in osteosarcoma models[7]. Doxorubicin is frequently used as an adjuvant chemotherapeutic agent for breast cancer. Silk films loaded with doxorubicin provide locoregional control of human breast cancer in vivo. By manipulating silk crystallinity or β-sheet content, the doxorubicin release rate could be controlled. Both soluble and stabilised silk films loaded with doxorubicin had a significantly greater primary tumour response than the equivalent dose of doxorubicin administered intravenously in the absence of the silk film carrier. The future use of this approach for localised chemotherapy is promising[8]

References:
[1].Escoffre JM, Piron J, et al. Doxorubicin delivery into tumor cells with ultrasound and microbubbles. Mol Pharm. 2011;8(3):799-806.
[2].Rhee HK, Park HJ, et al. Synthesis, cytotoxicity, and DNA topoisomerase II inhibitory activity of benzofuroquinolinediones. Bioorg Med Chem. 2007 Feb 15;15(4):1651-8.
[3].Foglesong PD, Reckord C, Swink S. Doxorubicin inhibits human DNA topoisomerase I. Cancer Chemother Pharmacol. 1992;30(2):123-5.
[4].Jie L, Lang D, et al. Superparamagnetic Iron Oxide Nanoparticles/Doxorubicin-Loaded Starch-Octanoic Micelles for Targeted Tumor Therapy. J Nanosci Nanotechnol. 2019;19(9):5456-5462.
[5].Soininen SK, Repo JK, et al. Human placental cell and tissue uptake of doxorubicin and its liposomal formulations. Toxicol Lett. 2015;239(2):108-114.
[6].Niu G, Cogburn B, et al. Preparation and characterization of doxorubicin liposomes. Methods Mol Biol. 2010;624:211-219.
[7].Seib FP, Kaplan DL. Doxorubicin-loaded silk films: drug-silk interactions and in vivo performance in human orthotopic breast cancer. Biomaterials. 2012;33(33):8442-8450.
[8]. Ma L, Xu Y, Xu X. Targeted MEK inhibition by cobimetinib enhances doxorubicin's efficacy in osteosarcoma models. Biochem Biophys Res Commun. 2020;529(3):622-628.