鹽酸伊達(dá)比星作用機(jī)制 - Medchemexpress - MCE中國

1、Product Data SheetIdarubicin hydrochlorideCat. No.: HY-17381CAS No.: 57852-57-0分式: CHClNO分量: 533.95作靶點: Topoisomerase; Bacterial; Fungal; Autophagy作通路: Cell Cycle/DNA Damage; Anti-infection; Autophagy儲存式: 4C, sealed storage, away from moisture and light* In solvent : -80C, 6 months; -20C, 1 month (s

2、ealed storage, away frommoisture and light)溶解性數(shù)據(jù)體外實驗 DMSO : 50 mg/mL (93.64 mM)H2O : 6.67 mg/mL (12.49 mM; Need ultrasonic)* means soluble, but saturation unknown.SolventMass1 mg 5 mg 10 mgConcentration制備儲備液1 mM 1.8728 mL 9.3642 mL 18.7283 mL5 mM 0.3746 mL 1.8728 mL 3.7457 mL10 mM 0.1873 mL 0.9364 m

3、L 1.8728 mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲備液的保存式和期限：-80C, 6 months; -20C, 1 month (sealed storage, away from moisture and light)。-80C儲存時，請在 6 個內(nèi)使，-20C 儲存時，請在 1 個內(nèi)使。體內(nèi)實驗請根據(jù)您的實驗動物和給藥式選擇適當(dāng)?shù)娜芙獍?。以下溶解案都請先按?In Vitro 式配制澄清的儲備液，再依次添加助溶劑：為保證實驗結(jié)果的可靠性，澄 的儲備液可以根據(jù)儲存條件，適當(dāng)保存；體內(nèi)實驗的作液，建議您現(xiàn)現(xiàn)配，

4、當(dāng)天使； 以下溶劑前顯的百分 指該溶劑在您配制終溶液中的體積占；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的式助溶1. 請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (4.68 mM); Clear solution此案可獲得 2.5 mg/mL (4.68 mM，飽和度未知) 的澄清溶液。以 1 mL 作液為例，取 100 L 25.0 mg/mL 的澄 DMSO 儲備液加到 400 L PEG300 中，混合均勻；向上述體系中加50 L Tween-80，混合均勻；然后繼續(xù)

5、加 450 L 理鹽定容 1 mL。2. 請依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (4.68 mM); Clear solutionPage 1 of 2 www.MedChemE此案可獲得 2.5 mg/mL (4.68 mM，飽和度未知) 的澄清溶液。以 1 mL 作液為例，取 100 L 25.0 mg/mL 的澄 DMSO 儲備液加到 900 L 20% 的 SBE-CD 理鹽溶液中，混合均勻。BIOLOGICAL ACTIVITY物活性 Idarubicin hydrochloride h

6、ydrochloride 還抑制細(xì)種蒽環(huán)類抗病藥物。 它抑制 拓?fù)洚悩?gòu)酶 II，擾 DNA 復(fù)制和 RNA 轉(zhuǎn)錄。Idarubicin和酵母 的長。IC & Target Topoisomerase II體外研究 The IC50 of idarubicin is 3.30.4 ng/mL on MCF-7 monolayers and 7.91.1 ng/mL in multicellular spheroids1.Idarubicin has shown a greater cytotoxicity than daunorubicin or doxorubicin in various i

7、n vitro systems. This hasbeen attributed to a better ability of idarubicin to induce the formation of topoisomerase II -mediated DNA breaks2.Idarubicin is about 57.5-fold and 25-fold more active than doxorubicin and epirubicin, respectively3. Idarubicinproduces a concentration-dependent reduction in

8、 cell growth, with an IC50 value of approximately 0.01 M.Idarubicin produced a concentration-dependent inhibition of DNA synthesis4.PROTOCOLCell Assay 1 Stock solutions of idarubicin hydrochloride is dissolved in distilled water (1 mg/mL). MCF-7 monolayer are exposed toidarubicin or its metabolite i

9、darubicinol at 0.01, 0.1, 1, 10, 100, and 1000 ng/mL for 24 hours. Multicellular spheroidsare exposed to the same range of idarubicin and idarubicinol concentration as monolayers (0.01-1000 ng/mL) for 24h and, in separate experiments, at the drug concentration of 100 ng/mL for 6, 12, 24 and 48 h. Th

10、e inhibition of cellproliferation is determined by counting the viable cells with an hemocytometer. Results are expressed as percentageof cell survival vs. control cultures1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.戶使本產(chǎn)品發(fā)表的科研獻(xiàn) Nucleic Acids Res.

11、2018 Apr 20;46(7):3284-3297. Cancer Lett. 2019 Jul 10;461:31-43. J Mol Med (Berl). 2019 Aug;97(8):1183-1193. J Virol. 2019 Mar 13. pii: JVI.02230-18. Exp Cell Res. 2020 May 3:112054.See more customer validations on HYPERLINK www.MedChemE www.MedChemEREFERENCES1. Orlandi P, et al. Idarubicin and idar

12、ubicinol effects on breast cancer multicellular spheroids. J Chemother. 2005 Dec;17(6):663-7.2. Robert J. Clinical pharmacokinetics of idarubicin. Clin Pharmacokinet. 1993 Apr;24(4):275-88.Page 2 of 3 www.MedChemE3. Siegsmund MJ, et al. Enhanced in vitro cytotoxicity of idarubicin compared to epirub

13、icin and doxorubicin in rat prostate carcinoma cells. Eur Urol.1997;31(3):365-70.4. Gewirtz DA, et al. Induction of DNA damage, inhibition of DNA synthesis and suppression of c-myc expression by the anthracycline analog, idarubicin (4-demethoxy-daunorubicin) in the MCF-7 breast tumor cell line. Cancer Chemother Pharmacol. 1998;41(5):361-5. Kinnunen U, et al. Idarubicin inhibits the growth of bacteria and yeasts in an automated blood culture system. Eur J Clin Microbiol Infect Dis. 2009Mar;28(3):301-3.McePdfHeightCauti