逆轉(zhuǎn)素作用機(jī)制 - Medchemexpress - MCE中國(guó)

1、Product Data SheetReversineCat. No.: HY-14711CAS No.: 656820-32-5分式: CHNO分量: 393.49作靶點(diǎn): Aurora Kinase; Autophagy作通路: Cell Cycle/DNA Damage; Epigenetics; Autophagy儲(chǔ)存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 20 mg/mL (50.83 mM; Need ultrasonic)H2O : 1.5 M and

2、 that the IC50 on muscle myosin (an analogue of nonmusclemyosin II) is 350 nM1.體內(nèi)研究 The combination of Reversine and aspirin can more efficiently induce cell cycle arrest and apoptosis. To evaluate theanti-tumor effect of this combination, a xenograft nude mouse model is established by s.c. injectio

3、n. Mice inoculatedwith cervical cancer cells have lost about 10 % of their initial body weight by about 16 days after tumor inoculation.However, tumor growth (tumor weight) is reduced and the mice survive longer in the combination group2.PROTOCOLCell Assay 1 HCT116 and HL60 cells are incubated with

4、either 5 mol/L Reversine or DMSO 0.01%. Cells are harvested and fixed in70% ethanol overnight. After double washing with PBS, cells are labeled with cell cycle staining reagent PBS, 0.1%Triton X-100, 200 g/mL DNase-free RNase, and 25 g/mL propidium iodide and incubated at room temperature inthe dark

5、 for 30 min. DNA content is analyzed using FACSCalibur. Cell viability of different tumor cell lines is assessedusing ATPlite 1step. Briefly, 2104 cells for each well are plated in a 96-well plate in presence of crescent quantity ofReversine. After 72 h, the plates are recovered and 100 L ATPlite so

6、lution is added to each well. The plates areshaken for 2 min at 700 rpm and luminescence is measured using EnVision Multilabel plate reader. Each sample isanalyzed in triplicate1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Mice2Administration

7、 2 Female athymic 6-8 weeks old BALB/c nude mice are used. U14 cell suspension (5106 cells in 100 L of RPMI-1640medium) is injected subcutaneously. The purpose of developing cervical tumors is to generate histological intacttumors for drug therapy. When the diameter of tumors reached up to about 1 c

8、m, Reversine, aspirin or theircombinations are administrated by intraperitoneal injection per 3 days, twenty-five of these mice are randomlyassigned into one of the following five groups: (a) mice treated with RPMI-1640 medium, (b) mice treated withDMSO, (c) mice treated with Reversine (10 mg/kg), (

9、d) mice treated with aspirin (1 g/kg) and (e) mice treated with aReversine and aspirin combination. Body weight and tumor size at the site of inoculation are measured three times aweek. Tumor size is measured every 3 days from two diameters, tumor volume is estimated using the formula LS2/2(L as the

10、 longest diameter, S as the shortest diameter).MCE has not independently confirmed the accuracy of these methods. They are for reference only.戶使本產(chǎn)品發(fā)表的科研獻(xiàn) Cell Rep. 2018 Nov 27;25(9):2317-2328.e5. J Biol Chem. 2019 Feb 8;294(6):2021-2035. Onco Targets Ther. 2018 Feb 26;11:1025-1035. Biochem Bioph Res

11、 Co. 2020 May 23. Chinese Pharmacological Bulletin, 2018, 34(12): 1740-1744.See more customer validations on HYPERLINK www.MedChemE www.MedChemEREFERENCES1. DAlise AM, et al. Reversine, a novel Aurora kinases inhibitor, inhibits colony formation of human acute myeloid leukemia cells. Mol Cancer Ther. 2008May;7(5):1140-9.Page 2 of 3 www.MedChemE2. Qin HX, et al. Synergistic antitumor activity of reversine combined with aspirin in cervical carcinoma in vitro and in vivo. Cytotechnology. 2013Aug;65(4):643-53.McePdfHeightCaution: Product has not been full