链脲霉素作用机制 - Medchemexpress - MCE中国

Product Data?SheetStreptozocinCat. No.:CAS No.:分?式:分?量:作?靶点:作?通路:储存?式:HY-1375318883-66-4C?H??N?O?265.22DNA/RNA Synthesis; DNA Alkylator/Crosslinker; Autophagy; BacterialCell Cycle/DNA Damage; Autophagy; Anti-infectionPowder-20°C4°C3 years2 yearsInhibitors?Agonists?Screening Libraries* 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 (490.16 mM; Need ultrasonic)H2O : 113.3 mg/mL (427.19 mM; Need ultrasonic and warming)Mass1 mg5 mg10 mgSolventConcentration制备储备液1 mM5 mM10 mM3.7705 mL0.7541 mL0.3770 mL18.8523 mL3.7705 mL1.8852 mL37.7045 mL7.5409 mL3.7705 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，澄清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?是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。 以 1 mL ?作液为例，取 100 μL 25.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加? 50 μL Tween-80，混合均匀；然后继续加? 450 μL ?理盐?定容? 1 mL。2. 请依序添加每种溶剂：?10% DMSO ?? 90% (20% SBE-β-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 μL 25.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD ?理盐??溶液中，混合Page 1 of 2 www.MedChemExpress.cn

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) 的澄清溶液，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 μL 25.8 mg/mL 的澄清 DMSO 储备液加到 900 μL ??油中，混合均匀。BIOLOGICAL ACTIVITY?物活性Streptozocin 是?种抗?素，可使 DNA 甲基化 (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体外研究DNA alkylator[1]Streptozocin (STZ) shows higher cytotoxic effect in vitro on hematological cell lines compared to Alloxan (ALX). ALX appeares not to be toxic for the studied cell lines with estimated IC50 values of 2809, 3679 or over 4000 μg/mL for HL60, K562 and C1498 cells, respectively. Streptozocin is more toxic, especially for the human myeloid leukemia cell line, HL60. The IC50 values of Streptozocin are 11.7, 904 and 1024 μg/mL for HL60, K562 and C1498 cells, respectively. Results also show that the murine leukemic cells are more resistant to Streptozocin and ALX cytotoxicity than human leukemic cells[2].体内研究Streptozocin (STZ)-injected mice show tendency to have lower body weight than that observed in animals injected with ALX. Streptozocin -injected mice have significantly fewer splenocytes (22.2±3.2×106; n=10) compared to mice injected with ALX (60.7±4.3×106; 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 2×104 cells/well in the absence (untreated control) or presence of various concentrations of ALX (20-3000 μg/mL) or STZ (1-3000 μg/mL) for 48 h at 37°C under a humidified atmosphere containing 5% CO2. Cells incubated in complete media including dH2O in a final concentration of 0.1% served as control for solvent toxicity and cells incubated in complete medium are used as a control for the experiments. The effects of the tested drugs on tumor cell growth or viability are determined employing the MTT assay in accordance with the manufacturer's instructions. The IC50values (drug concentration that induces 50% inhibition of the cell growth) are calculated using the GraphPad Prism 4 program[2].MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Administration [2][3]Mice[2] Male C57BL/6 mice (10-16 weeks) are used.The age group distribution in the mouse group treated with Streptozocin and ALX as well as controls is as follows: Streptozocin xenograft (n=7, median age 14 weeks), ALX xenograft (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 (75 mg/mL) or Streptozocin (180 mg/kg). Control group contain male C57BL/6 mice. Blood glucose levels and body weight are measured before injection, after 6 h, then daily after drug injection. Rats[3] Thirty rats underwent oophorectomy to induce menopausal status. Rats receive intraperitoneal administration of Streptozocin (50 mg/kg) to induce diabetes mellitus (DM) 1 week after the oophorectomy. Blood glucose level is checked 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

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????Nat Biomed Eng. 2020 May;4(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 www.MedChemExpress.cnREFERENCES

[1].?Bennett RA, et al. Alkylation of DNA in rat tissues following administration of streptozotocin. Cancer Res. 1981 Jul;41(7):2786-90

[2].?Diab RA, et al. Immunotoxicological effects of streptozotocin and alloxan: in vitro and in vivo studies. Immunol Lett. 2015 Feb;163(2):193-8[3].?Acer S, et al. Oxidative stress of crystalline lens in rat menopausal model. Arq Bras Oftalmol. 2016 Jul-Aug;79(4):222-5.

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