槲皮素作用机制 - Medchemexpress - MCE中国

1、Product Data SheetQuercetinCat. No.: HY-18085CAS No.: 117-39-5分式: CHO分量: 302.24作靶点: PI3K; Autophagy; Mitophagy; Apoptosis作通路: PI3K/Akt/mTOR; Autophagy; Apoptosis储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 100 mg/mL (330.86 mM)* means soluble, but saturation

2、 unknown.SolventMass1 mg 5 mg 10 mgConcentration制备储备液1 mM 3.3086 mL 16.5431 mL 33.0863 mL5 mM 0.6617 mL 3.3086 mL 6.6173 mL10 mM 0.3309 mL 1.6543 mL 3.3086 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；旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存式和期限：-80C, 6 months; -20C, 1 month。-80C 储存时，请在 6 个内使，-20C 储存时，请在 1 个内使。体内实验请根据您的实验

3、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 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: 2.5 mg/mL (8.27 mM); Clear solution此案可获得 2.5 mg/mL (8.27 mM，饱和度未知)

4、的澄清溶液。以 1 mL 作液为例，取 100 L 25.0 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: 2.5 mg/mL (8.27 mM); Clear solutionPage 1 of 2 www.MedChemE此案可获得 2.5 mg/mL (8.27 mM，饱和度未知) 的澄清溶液。以 1 mL 作液为例，取 100 L 25.

5、0 mg/mL 的澄 DMSO 储备液加到 900 L 20% 的 SBE-CD 理盐溶液中，混合均匀。BIOLOGICAL ACTIVITY物活性 Quercetin 种天然 酮类化合物，可激活或抑制许多蛋质的活性。 槲素可激活SIRT1，也可抑制 PI3K，抑制 PI3K ，PI3K ，PI3K 的 IC50 分别为2.4 M, 3.0 M, 5.4 M。IC & Target PI3K PI3K PI3K Autophagy5.4 M (IC50) 2.4 M (IC50) 3 M (IC50)Mitophagy体外研究 Quercetin is a type of plant-base

6、d chemical, or phytochemical, used as an ingredient in supplements, beverages orfoods. In several studies, it may have anti-inflammatory and antioxidant properties, and it is being investigated for awide range of potential health benefits. Quercetin is a PI3K inhibitor with IC50 of 2.4-5.4 M. Querce

7、tin stronglyabrogates PI3K and Src kinases, mildly inhibits Akt1/2, and slightly affected PKC, p38 and ERK1/21. Quercetin inhibitsTNF-induced LDH% release, EC-dependent neutrophils adhesion to bovine pulmonary artery endothelial cells(BPAEC), and BPAEC DNA synthesis and proliferation2.体内研究 Combinati

8、on of Quercetin (75 mg/kg) and 2-Methoxyestradiol enhances inhibition of human prostate cancer LNCaPand PC-3 cells xenograft tumor growth3.PROTOCOLAnimal Mice are inoculated subcutaneously with 5105 PC-3 cells suspended in 100L PBS and 2108 LNCaP cellsAdministration 3 suspended in 100L of matrigel a

9、nd PBS mixture (1:1) on the right back. When xenograft tumors reach a volume ofapproximately 100 mm3, mice are randomLy assigned to four groups (n=8 each group) and treated intraperitoneally.Therapeutic schedule based on our in vitro results, preliminary experiments and many other researchers studie

10、s is asfollows: (1) Vehicle control group: vehicle of quercetin on day 1, vehicle of 2-ME on day 2, (2) Quercetin treatedgroup: quercetin 75 mg/kg on day 1, vehicle of 2-ME on day 2, (3) 2-ME treated group: vehicle of quercetin on day 1,2-ME 150 mg/kg on day 2, (4) Combination treatment group: querc

11、etin 75 mg/kg on day 1, 2-ME 150 mg/kg on day2. Two days is a treatment cycle and the whole treatment process lasted for 4 weeks. Tumor sizes are monitoredevery 2 days using caliper and tumor volume are calculated according to the formula: LS20.5, in which Lrepresents the longest diameter and S repr

12、esents the shortest diameter of tumor. Mice are weighed as well. At theend of treatment procedure, on day 29, mice are anesthetized with chloral hydrate and sacrificed by cervicaldislocation. Xenograft tumors are taken out quickly and weighed. One part of it is put into liquid nitrogenimmediately fo

13、r future biomarker analysis and the other part is fixed in 10% neutral buffered formalin forimmunohistochemical analysis. Serum biochemical parameters such as ALT, AST, creatinine and urea nitrogen thatreflected drug toxicity are also detected.MCE has not independently confirmed the accuracy of thes

14、e methods. They are for reference only.户使本产品发表的科研献Page 2 of 3 www.MedChemE Eur J Med Chem. 2018 Mar 25;148:63-72. Exp Cell Res. 2020 May 3:112054. Molecules. 2020 Apr 23;25(8). pii: E1980. Insects. 2018 Jun 29;9(3). pii: E77. Int J Insect Sci. 2018 Feb 28;10:1179543318758409.See more customer valida

15、tions on HYPERLINK www.MedChemE www.MedChemEREFERENCES1. Navarro-N?ez L, et al. Effect of quercetin on platelet spreading on collagen and fibrinogen and on multiple platelet kinases. Fitoterapia. 2010Mar;81(2):75-80.2. Yu XB, et al. Inhibitory effects of protein kinase C inhibitors on tumor necrosis factor induced bovine pulmonary artery endothelial cell injuries. Yao XueXue Bao. 1996;31(3):176-81.3. Yang F, et al. Combination of Quercetin and 2-Methoxyestradiol Enhances Inhibition of Human Prostate Cancer LNCaP and PC-3 Cells Xenograft TumorGrowth. PLoS One. 2015 May