鏈脲霉素作用機(jī)制 - Medchemexpress - MCE中國(guó)

1、Product Data SheetStreptozocinCat. No.: HY-13753CAS No.: 18883-66-4分式: CHNO分量: 265.22作靶點(diǎn): DNA/RNA Synthesis; DNA Alkylator/Crosslinker; Autophagy; Bacterial作通路: Cell Cycle/DNA Damage; Autophagy; Anti-infection儲(chǔ)存式: Powder -20C 3 years4C 2 years* 該產(chǎn)品在溶液狀態(tài)不穩(wěn)定，建議您現(xiàn)現(xiàn)配，即刻使。溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 130 mg/mL (490.

2、16 mM; Need ultrasonic)H2O : 113.3 mg/mL (427.19 mM; Need ultrasonic and warming)SolventMass1 mg 5 mg 10 mgConcentration制備儲(chǔ)備液1 mM 3.7705 mL 18.8523 mL 37.7045 mL5 mM 0.7541 mL 3.7705 mL 7.5409 mL10 mM 0.3770 mL 1.8852 mL 3.7705 mL請(qǐng)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(chǔ)備液；該產(chǎn)品在溶液狀態(tài)不穩(wěn)定，建議您現(xiàn)現(xiàn)配，即刻使.體內(nèi)實(shí)驗(yàn)請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥式選

3、擇適當(dāng)?shù)娜芙獍?。以下溶解案都?qǐng)先按照 In Vitro 式配制澄清的儲(chǔ)備液，再依次添加助溶劑：為保證實(shí)驗(yàn)結(jié)果的可靠性，澄 的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的作液，建議您現(xiàn)現(xiàn)配，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(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)加熱和/或超聲的式助溶1. 請(qǐng)依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.58 mg/mL (9.73 mM); Clear solution此案可獲得 2.58 mg/mL (9.73 mM，飽和度未知) 的澄清溶液

4、。以 1 mL 作液為例，取 100 L 25.8 mg/mL 的澄 DMSO 儲(chǔ)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)加 450 L 理鹽定容 1 mL。2. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.58 mg/mL (9.73 mM); Clear solution此案可獲得 2.58 mg/mL (9.73 mM，飽和度未知) 的澄清溶液。以 1 mL 作液為例，取 100 L 25.8 mg/mL 的澄 DMSO 儲(chǔ)備液加到 900 L

5、 20% 的 SBE-CD 理鹽溶液中，混合Page 1 of 2 www.MedChemE均勻。3. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.58 mg/mL (9.73 mM); Clear solution此案可獲得 2.58 mg/mL (9.73 mM，飽和度未知) 的澄 溶液，此案不適于實(shí)驗(yàn)周 期在半個(gè)以上的實(shí)驗(yàn)。以 1 mL 作液為例，取 100 L 25.8 mg/mL 的澄 DMSO 儲(chǔ)備液加到 900 L 油中，混合均勻。BIOLOGICAL ACTIVITY物活性 Streptozocin種抗素，可使 DNA 甲基化 (

6、DNA-methylating) 。Streptozocin 引起肝臟，腎臟及胰腺 DNA 甲基化，但腦 DNA 中沒(méi)有甲基化。IC & Target DNA alkylator1體外研究 Streptozocin (STZ) shows higher cytotoxic effect in vitro on hematological cell lines compared to Alloxan (ALX). ALXappeares not to be toxic for the studied cell lines with estimated IC50 values of 2809, 3

7、679 or over 4000 g/mL forHL60, K562 and C1498 cells, respectively. Streptozocin is more toxic, especially for the human myeloid leukemia cellline, HL60. The IC50 values of Streptozocin are 11.7, 904 and 1024 g/mL for HL60, K562 and C1498 cells, respectively.Results also show that the murine leukemic

8、 cells are more resistant to Streptozocin and ALX cytotoxicity than humanleukemic cells2.體內(nèi)研究 Streptozocin (STZ)-injected mice show tendency to have lower body weight than that observed in animals injectedwith ALX. Streptozocin -injected mice have significantly fewer splenocytes (22.23.2106; n=10) c

9、ompared to mice injected with ALX (60.74.3106; n=15; p=0.01)2.PROTOCOLCell Assay 2 Human and murine cell lines are cultured in triplicate in 96-well plates at a density of 2104 cells/well in the absence(untreated control) or presence of various concentrations of ALX (20-3000 g/mL) or STZ (1-3000 g/m

10、L) for 48 h at37C under a humidified atmosphere containing 5% CO2. Cells incubated in complete media including dH2O in afinal concentration of 0.1% served as control for solvent toxicity and cells incubated in complete medium are used asa control for the experiments. The effects of the tested drugs

11、on tumor cell growth or viability are determinedemploying the MTT assay in accordance with the manufacturers instructions. The IC50values (drug concentration thatinduces 50% inhibition of the cell growth) are calculated using the GraphPad Prism 4 program2.MCE has not independently confirmed the accu

12、racy of these methods. They are for reference only.Animal Mice2Administration 23 Male C57BL/6 mice (10-16 weeks) are used.The age group distribution in the mouse group treated with Streptozocinand ALX as well as controls is as follows: Streptozocin xenograft (n=7, median age 14 weeks), ALX xenograft

13、 (n=11,median age 15 weeks), Streptozocin non-transplanted (n=7, median age 14 weeks), ALX non-transplanted (n=15,median age 15 weeks).Male C57BL/6 mice are under inhalation anesthesia injected via the penile vein with ALX (75mg/mL) or Streptozocin (180 mg/kg). Control group contain male C57BL/6 mic

14、e. Blood glucose levels and bodyweight are measured before injection, after 6 h, then daily after drug injection.Rats3Thirty rats underwent oophorectomy to induce menopausal status. Rats receive intraperitoneal administration ofStreptozocin (50 mg/kg) to induce diabetes mellitus (DM) 1 week after th

15、e oophorectomy. Blood glucose level ischecked 3 days after Streptozocin administration, and values 250 mg/dL are considered as positive for DM.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Page 2 of 3 www.MedChemE戶(hù)使本產(chǎn)品發(fā)表的科研獻(xiàn) Nat Biomed Eng. 2020 May;4

16、(5):507-517. J Mol Med (Berl). 2019 Aug;97(8):1183-1193. Heliyon. 2020 May. bioRxiv. 2020 Feb. Chinese Journal of Clinical Pharmacoly and Therapeutics. 2017, 22(8): 846-851.See more customer validations on HYPERLINK www.MedChemE www.MedChemEREFERENCES1. Bennett RA, et al. Alkylation of DNA in rat ti

17、ssues following administration of streptozotocin. Cancer Res. 1981 Jul;41(7):2786-902. Diab RA, et al. Immunotoxicological effects of streptozotocin and alloxan: in vitro and in vivo studies. Immunol Lett. 2015 Feb;163(2):193-83. Acer S, et al. Oxidative stress of crystalline lens in rat menopausal model. Arq Bras