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1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEStreptozocinCat. No.: HY-13753CAS No.: 18883-66-4Synonyms: Streptozotocin; U 9889分式: CHNO分量: 265.22作靶點: DNA/RNA Synthesis; DNA Alkylator/Crosslinker; Autophagy;Bacterial作通路: Cell Cycle/DNA Damage; Autophagy; Anti-infection儲存式: P
2、owder -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)體外實驗 H2O : 113.3 mg/mL (427.19 mM; Need ultrasonic and warming)DMSO : 30 mg/mL (113.11 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 3.7705 mL 18.8523 mL 37.7045 mL5 mM 0.7541 mL 3.7705 mL 7.540
3、9 mL10 mM 0.3770 mL 1.8852 mL 3.7705 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;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)實驗請根據(jù)您的實驗動物和給藥式選擇適當?shù)娜芙獍?,配制前請先配制澄清的儲備液,再依次添加助溶?為保證實驗結果的可靠性,體內(nèi)實驗的作液,建議您現(xiàn)現(xiàn)配,當天使;澄清的儲備液可以根據(jù)儲存條件,適當保存;以下溶劑前的百分 指該溶劑在您配制終溶液中的體積占):1. 請依序添加每種溶劑: 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.58 mg/mL (9.
4、73 mM); Clear solution1/3 Master of Small Molecules 您邊的抑制劑師www.MedChemE2. 請依序添加每種溶劑: 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.58 mg/mL (9.73 mM); Clear solution3. 請依序添加每種溶劑: 10% DMSO 90% corn oilSolubility: 2.58 mg/mL (9.73 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Streptozocin種抗素,可使 DNA 甲基化
5、 (DNA-methylating) 。Streptozocin 引起肝臟,腎臟及胰腺DNA 甲基化,但腦 DNA 中沒有甲基化。IC50 & Target DNA alkylator 1體外研究 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 280
6、9, 3679 orover 4000 g/mL for HL60, K562 and C1498 cells, respectively. Streptozocin is more toxic, especially for thehuman myeloid leukemia cell line, HL60. The IC50 values of Streptozocin are 11.7, 904 and 1024 g/mL forHL60, K562 and C1498 cells, respectively. Results also show that the murine leuk
7、emic cells are moreresistant to Streptozocin and ALX cytotoxicity than human leukemic cells 2.體內(nèi)研究 Streptozocin (STZ)-injected mice show tendency to have lower body weight than that observed in animalsinjected with ALX. Streptozocin -injected mice have significantly fewer splenocytes (22.23.2106; n=
8、10)compared 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 theabsence (untreated control) or presence of various concentrations of ALX (20-3000 g/mL) or STZ (1-300
9、0 g/mL) for 48 h at 37C under a humidified atmosphere containing 5% CO2. Cells incubated in completemedia including dH2O in a final concentration of 0.1% served as control for solvent toxicity and cellsincubated in complete medium are used as a control for the experiments. The effects of the tested
10、drugs ontumor cell growth or viability are determined employing the MTT assay in accordance with the manufacturersinstructions. The IC50values (drug concentration that induces 50% inhibition of the cell growth) arecalculated using the GraphPad Prism 4 program 2.MCE has not independently confirmed th
11、e accuracy of these methods. They are for reference only.Animal Mice 2Administration 23 Male C57BL/6 mice (10-16 weeks) are used.The age group distribution in the mouse group treated withStreptozocin and ALX as well as controls is as follows: Streptozocin xenograft (n=7, median age 14 weeks),ALX xen
12、ograft (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 anesthesiainjected via the penile vein with ALX (75 mg/mL) or Streptozocin (180 mg/kg). Control group contain maleC57BL
13、/6 mice. Blood glucose levels and body weight are measured before injection, after 6 h, then daily2/3 Master of Small Molecules 您邊的抑制劑師www.MedChemEafter drug injection.Rats 3Thirty rats underwent oophorectomy to induce menopausal status. Rats receive intraperitoneal administrationof Streptozocin (50
14、 mg/kg) to induce diabetes mellitus (DM) 1 week after the oophorectomy. Blood glucoselevel is checked 3 days after Streptozocin administration, and values 250 mg/dL are considered as positivefor DM.MCE has not independently confirmed the accuracy of these methods. They are for reference only.戶使本產(chǎn)品發(fā)表
15、的科研獻 J Mol Med (Berl). 2019 Jun 14. Chinese Journal of Clinical Pharmacoly and Therapeutics. 2017, 22(8): 846-851.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Bennett RA, et al. Alkylation of DNA in rat tissues 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. 2015Feb;163(2):193-83. Acer S, et al. Oxidative stress of crystalline lens in rat menopausal model. Arq Bra
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