Daunorubicin hydrochloride
作者：齐岳
发布时间：2023-09-13
17:40:28
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产品名称：Daunorubicin hydrochloride
产品描述：
| 植物来源 | 天然产物 > 其他（植物来源） > 其他 |
| 产品描述 | Daunorubicin hydrochloride, an anthracycline aminoglycoside antineoplastic, inhibits DNA replication and repair and RNA and protein synthesis. |
| 靶点活性 | DNA synthesis:20 nM(Ki) |
| 体外活性 | At drug concentrations that reflect the peak plasma concentration after Daunorubicin administration, the primary mechanism is likely to be through interaction with topoisomerase II, which may be a primary triggering event for growth arrest and/or cell killing through a signalling pathway leading to apoptosis, at least in leukemic cells and thymocytes. The quinone structure permits daunorubicin to act as electron acceptors in reactions mediated by oxoreductive enzymes including cytochrome P450 reductase, NADH dehydrogenase, and xanthine oxidase. At Daunorubicin concentrations exceeding approximately 2–4 μM, free radical mediated toxicity and DNA cross-linking may become evident. Daunorubicin inhibits both DNA and RNA syntheses in HeLa cells over a concentration range of 0.2 through 2 μM. Daunorubicin inhibits both DNA syntheses in Ehrlich ascites tumor cells over a concentration range of 4 μM. Daunorubic triggers apoptosis at concentrations of 0.5 and 1 μM in either HL-60 or U-937 human leukemic cells. [1] Daunorubicin stimulates ceramide elevation and apoptosis in P388 and U937 cells through de novo synthesis via activation of the enzyme ceramide synthase. [2] Daunorubicin dose-dependently increases the phosphatidylserine exposure and consequent procoagulant activity of human umbilical vein endothelial cells. Daunorubicin (0.2 mM) significantly enhances the release of endothelial microparticles which are highly procoagulant in human umbilical vein endothelial cells. [3] |
| 体内活性 | Urinary protein excretion, serum creatinine, and blood urea nitrogen (BUN) level are significantly increased in group Daunorubicin (3 mg/kg, i.v.) compared with those in group Control. Administration of Daunorubicin (DNR) causes a significant increase in malondialdehyde (MDA) level in renal tissue compared with that in the control group[5]. |
| 细胞实验 | Daunorubicin (Dnr) is prepared in PBS[2]. The chemosensitivity to Daunorubicin is assessed using the MTT assay. In brief, the 96 well plates are set up with cells at the initial density of 2×105 cells/mL and are incubated at 37°C for 72 h in an atmosphere of 5% CO2 in the absence and presence of nine different concentrations of Daunorubicin (Dnr) or Dox ranging from 1.90 to 0.007 μM in triplicate. After incubation, 10 μL of MTT solution (5 mg/mL tetrazolium salt) is added to each well and the plates are incubated for a further 4 h at 37°C. The formazan salt crystals are dissolved by adding 100 μL 10% SDS in 10 mM HCl solution and incubating over night at 37°C. The absorbance is measured at 540 nm with a reference at 650 nm by a 96-well enzyme-linked immunosorbent assay (ELISA) plate reader. Chemosensitivity is expressed as the IC50, which is the concentration of drug causing 50% cell survival compare to control cells grown without drug. Calculations are carried out using Microsoft Excel[2]. |
| 别名 | Daunomycin HCl, Daunorubicin HCl, 盐酸佐柔比星, 盐酸柔红霉素, Daunomycin, RP-13057 Hydrochloride, Rubidomycin hydrochloride |
| 分子量 | 563.99 |
| 分子式 | C27H29NO10·HCl |
| CAS No. | 23541-50-6 |
存储
Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
H2O: 92 mg/mL (163.1 mM)
DMSO: 93 mg/mL (164.9 mM)
Ethanol: <1 mg/mL
( < 1 mg/mL refers to the product slightly soluble or insoluble )
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