1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEDaunorubicin HydrochlorideCat. No.: HY-13062CAS No.: 23541-50-6Synonyms: RP 13057 (Hydrochloride); Daunomycin (Hydrochloride);Rubidomycin (Hydrochloride)分式: CHClNO分量: 563.98作靶點: Topoisomerase; DNA/RNA Synthesis; ADC Cytotoxin;Au

2、tophagy作通路: Cell Cycle/DNA Damage; Antibody-drug Conjugate/ADCRelated; Autophagy儲存式: 4C, protect from light* In solvent : -80C, 6 months; -20C, 1 month (protect fromlight)溶解性數據體外實驗 H2O : 34 mg/mL (60.29 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 1.7

3、731 mL 8.8656 mL 17.7311 mL5 mM 0.3546 mL 1.7731 mL 3.5462 mL10 mM 0.1773 mL 0.8866 mL 1.7731 mL請根據產品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存式和期限。BIOLOGICAL ACTIVITY物活性 Daunorubicin Hydrochloride (RP 13057 Hydrochloride)是具有有效抗腫瘤活性的 DNA拓撲異構酶II。Daunorubicin Hydrochloride (RP 13057 Hydrochloride) 抑制敏感和耐藥的埃利腹

4、腫瘤細胞的 DNA 和RNA 合成。1/3 Master of Small Molecules 您邊的抑制劑師www.MedChemEIC50 & Target Topoisomerase II體外研究 The mean IC50 value is 0.04 M for Daunorubicin Hydrochloride (RP 13057 Hydrochloride) in Molt-4 cells.Daunorubicin Hydrochloride (RP 13057 Hydrochloride) belongs to the anthracyclines, a group of cy

5、totoxicchemotherapeutics. The cytotoxic effects of anthracyclines are caused by DNA intercalation and the ability tointerfere with DNA transcription and replication by inhibiting Topoisomerase II as well as by producingreactive oxygen species 2.Daunorubicin Hydrochloride (RP 13057 Hydrochloride) inh

6、ibits of both DNA and RNA synthesis in HeLa cellsover a concentration range of 0.2 through 2 M. The IC50 value is 0.4 M for Daunorubicin Hydrochloride(RP 13057 Hydrochloride) in human pancreatic cell line L3.6 3.體內研究 Urinary protein excretion, serum creatinine, and blood urea nitrogen (BUN) level ar

7、e significantly increased ingroup Daunorubicin Hydrochloride (RP 13057 Hydrochloride) (3 mg/kg, i.v.) compared with those in groupControl. Administration of Daunorubicin (DNR) causes a significant increase in malondialdehyde (MDA) levelin renal tissue compared with that in the control group 4.PROTOC

8、OLCell Assay 2 The chemosensitivity to Daunorubicin is assessed using the MTT assay. In brief, the 96 well plates are set upwith cells at the initial density of 2105 cells/mL and are incubated at 37C for 72 h in an atmosphere of 5%CO2 in the absence and presence of nine different concentrations of D

9、aunorubicin (Dnr) or Dox ranging from1.90 to 0.007 M in triplicate. After incubation, 10 L of MTT solution (5 mg/mL tetrazolium salt) is added toeach well and the plates are incubated for a further 4 h at 37C. The formazan salt crystals are dissolved byadding 100 L 10% SDS in 10 mM HCl solution and

10、incubating over night at 37C. The absorbance ismeasured 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% cellsurvival compare to control cells grown witho

11、ut drug. Calculations are carried out using Microsoft Excel 2.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Rat 4Administration 4 Eight-week-old male Sprague-Dawley rats are used. The animals are quarantined and acclimatized for theadditional 2

12、 weeks prior to the initiation of the experiments. On day 0, each animal receives a singleintravenous injection of Daunorubicin at a dose of 3 mg/kg (i.v.). Daunorubicin is administered in three equalinjections at 48 h intervals for a period of one week to achieve an accumulative dose of 9 mg/kg, wh

13、ich iswell documented to produce cardiotoxicity and nephrotoxicity. Age-matched rats are injected withcorresponding volumes of 0.9% NaCl and used as a control (group Control;n=5). Twenty-two DNR-treatedrats are randomly divided into two groups and received oral administration of Telmisartan (10 mg/k

14、g/day;group Daunorubicin+Telmisartan; n=10) or vehicle (group Daunorubicin; n=12). The dose of Telmisartan ischosen on the basis of a previous report. Administration of Telmisartan is started on the same day asDaunorubicin administration and continued for 5 additional weeks after cessation of Daunor

15、ubicinadministration (6 weeks total period). This duration of study is chosen on the basis of previous reports. Onday 41, rats are placed individually in metabolic cages for 24-h urine collections for the measurement ofprotein concentrations and body weight (BW) is measured. After the end of the stu

16、dy period (6 weeks), rats2/3 Master of Small Molecules 您邊的抑制劑師www.MedChemEare sacrificed and kidney tissue is harvested for semi-quantitative immunoblotting and immunohistochemicalstudies.MCE has not independently confirmed the accuracy of these methods. They are for reference only.戶使本產品發(fā)表的科研獻 J Mol

17、 Med (Berl). 2019 Jun 14. Curr Pharm Anal. 2018 Jan, 14(1):53-59(7).See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Lehmann M, et al. Activity of topoisomerase inhibitors daunorubicin, idarubicin, and aclarubicin in the Drosophila Somatic Mutation andRecombination Test. Environ

18、 Mol Mutagen. 2004;43(4):250-7.2. Svensson SP, et al. Melanin inhibits cytotoxic effects of Doxorubicin and Daunorubicin in MOLT 4 cells. Pigment Cell Res. 2003Aug;16(4):351-43. Gervasoni JE Jr, et al. An effective in vitro antitumor response against human pancreatic carcinoma with paclitaxel and Daunorubicin byinduction of both necrosis and apoptosis. Anticancer Res. 2004 Sep-Oct;24(5A):2617-264. Arozal W, et al