Isorhamnetin-3-Methylquercetin-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEIsorhamnetinCat. No.: HY-N0776CAS No.: 480-19-3Synonyms: 3-Methylquercetin分式: CHO分量: 316.26作靶点: MEK; PI3K作通路: MAPK/ERK Pathway; PI3K/Akt/mTOR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 :

2、28 mg/mL (88.53 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 3.1620 mL 15.8098 mL 31.6196 mL5 mM 0.6324 mL 3.1620 mL 6.3239 mL10 mM 0.3162 mL 1.5810 mL 3.1620 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，并请注意储备液的保存式和期限。BIOLOGICAL ACTIVITY物活性 Isorhamnetin是从中草药沙棘 (Hi

3、ppophae rhamnoides L.) 中提取的类黄酮化合物。Isorhamnetin 可通过直接抑制 MEK1 和 PI3K 来抑制肤癌。IC50 & Target MEK1 PI3-K1/3 Master of Small Molecules 您边的抑制剂师www.MedChemE体外研究 Isorhamnetin is a plant flavonoid that occurs in fruits and medicinal herbs. Isorhamnetin binds directly toMEK1 in an ATP-noncompetitive manner and t

4、o PI3-K in an ATP-competitive manner. In vitro and ex vivokinase assay data show that Isorhamnetin inhibits the kinase activity of MAP/ERK kinase (MEK) 1 and PI3-Kand the inhibition is due to direct binding with Isorhamnetin 1. Isorhamnetin inhibits the Akt/mTOR andMEK/ERK signaling pathways, and pr

5、omotes the activity of the mitochondrial apoptosis signaling pathway.The inhibitory effects of Isorhamnetin on breast cancer cells are determined using the CCK-8 method.Isorhamnetin inhibits the proliferation of numerous breast cancer cells (IC50, 10 M), including MCF7,T47D, BT474, BT-549, MDA-MB-23

6、1 and MDA-MB-468, whereas less inhibitory activity is observed in theMCF10A normal breast epithelial cell line (IC50, 38 M) 2.体内研究 Photographic data shows that Isorhamnetin treatment suppresses tumor development in mice. The averagevolume of tumors in untreated mice increases over time and reaches a

7、 volume of 623 mm3 at 4 weeks post-inoculation; however, at this time, in mice treated with 1 or 5 mg/kg Isorhamnetin, the average tumor volumeis only 280 or 198 mm3, respectively. At the end of the study, Isorhamnetin treatment (1 or 5 mg/kg) reducestumor weight compared with the untreated control

8、group 1.PROTOCOLCell Assay 2 MCF7, T47D, BT474, BT-549, MDA-MB-231 and MDA-MB-468 breast cancer cell lines, as well as aMCF10A normal breast epithelial cell line (control) are seeded into 96-well plates at a density of 5103cells/well in 100 L DMEM and placed in cell incubator for 12 h at 37C in an a

9、tmosphere containing 5%CO2. The cells are then treated with various concentrations of Isorhamnetin (100, 33.3, 11.1, 3.7, 1.2, 0.4and 0 M) for 48 h, and cell proliferation rates are determined by adding 10 L CCK-8 solution prior toincubation at 37C for 2 h. The absorbance is measured at a wavelength

10、 of 450 nm using a SpectraMax 190Microplate Reader. For each assay, four parallel wells are included, and the half maximal inhibitoryconcentration (IC50) is measured using the inhibition curve and presented as the mean of three independentexperiments 2.MCE has not independently confirmed the accurac

11、y of these methods. They are for reference only.Animal Mice 1Administration 1 Female athymic nude mice are injected subcutaneously in the flank with A431 cells (1106 cells in 50 L ofmedium and 50 L of Matrigel). Cells are allowed to form tumors, and once the tumors reach a size of 40mm3, the mice ar

12、e randomly assigned into groups (6 mice/group) and treated with (1 or 5 mg/kg bodyweight) or without Isorhamnetin in 40% DMSO/PBS buffer, administered intraperitoneally every other day for28 days. Tumor size is measured every week with calipers, and the tumor volume is calculated. Mice aresacrificed

13、 after 28 days of treatment when the control tumors reach approximately 600 mm3. The tumors areharvested, photographed, and weighed. Tumor tissues are used for western blot analysis andimmunohistochemical analysis.MCE has not independently confirmed the accuracy of these methods. They are for refere

14、nce only.REFERENCES2/3 Master of Small Molecules 您边的抑制剂师www.MedChemE1. Kim JE, et al. Isorhamnetin suppresses skin cancer through direct inhibition of MEK1 and PI3-K. Cancer Prev Res (Phila). 2011Apr;4(4):582-91.2. Hu S, et al. Isorhamnetin inhibits cell proliferation and induces apoptosis in breast cancer via Akt and mitogen activated protein kinasekinase signaling pathways. Mol Med Rep. 2015 Nov;