链脲霉素作用机制 - Medchemexpress - MCE中国

1、Product Data SheetStreptozocinCat. No.: HY-13753CAS No.: 18883-66-4分式: CHNO分量: 265.22作靶点: DNA/RNA Synthesis; DNA Alkylator/Crosslinker; Autophagy; Bacterial作通路: Cell Cycle/DNA Damage; Autophagy; Anti-infection储存式: Powder -20C 3 years4C 2 years* 该产品在溶液状态不稳定，建议您现现配，即刻使。溶解性数据体外实验 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制备储备液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请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液；该产品在溶液状态不稳定，建议您现现配，即刻使.体内实验请根据您的实验动物和给药式选

3、择适当的溶解案。以下溶解案都请先按照 In Vitro 式配制澄清的储备液，再依次添加助溶剂：为保证实验结果的可靠性，澄 的储备液可以根据储存条件，适当保存；体内实验的作液，建议您现现配，当天使； 以下溶剂前显的百分 指该溶剂在您配制终溶液中的体积占；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的式助溶1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.58 mg/mL (9.73 mM); Clear solution此案可获得 2.58 mg/mL (9.73 mM，饱和度未知) 的澄清溶液

4、。以 1 mL 作液为例，取 100 L 25.8 mg/mL 的澄 DMSO 储备液加到 400 L PEG300 中，混合均匀；向上述体系中加50 L Tween-80，混合均匀；然后继续加 450 L 理盐定容 1 mL。2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.58 mg/mL (9.73 mM); Clear solution此案可获得 2.58 mg/mL (9.73 mM，饱和度未知) 的澄清溶液。以 1 mL 作液为例，取 100 L 25.8 mg/mL 的澄 DMSO 储备液加到 900 L

5、 20% 的 SBE-CD 理盐溶液中，混合Page 1 of 2 www.MedChemE均匀。3. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.58 mg/mL (9.73 mM); Clear solution此案可获得 2.58 mg/mL (9.73 mM，饱和度未知) 的澄 溶液，此案不适于实验周 期在半个以上的实验。以 1 mL 作液为例，取 100 L 25.8 mg/mL 的澄 DMSO 储备液加到 900 L 油中，混合均匀。BIOLOGICAL ACTIVITY物活性 Streptozocin种抗素，可使 DNA 甲基化 (

6、DNA-methylating) 。Streptozocin 引起肝脏，肾脏及胰腺 DNA 甲基化，但脑 DNA 中没有甲基化。IC & Target DNA alkylator1体外研究 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.体内研究 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户使本产品发表的科研献 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