1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEArtesunateCat. No.: HY-N0193CAS No.: 88495-63-0分式: CHO分量: 384.42作靶點(diǎn): STAT作通路: JAK/STAT Signaling; Stem Cell/Wnt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 : 83.33 mg/mL (216.77 mM; Need u

2、ltrasonic)H2O : 40% PEG300 5% Tween-80 45% salineSolubility: 2.08 mg/mL (5.41 mM); Clear solution2. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.08 mg/mL (5.41 mM); Clear solution3. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% corn oil1/3 Master of Small Molecules 您邊的抑制劑師www.MedChemESolubility: 2.08 mg/mL

3、 (5.41 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 ArtesunateSTAT-3 和輸出蛋 1 (EXP1) 的抑制劑。IC50 & Target Stat-3 EXP1體外研究 Artesunate is an inhibitor of both STAT-3 1 and exported protein 1 (EXP1) 2. Artesunate treatment for 24 hcauses a significant increase in the levels of reactive oxygen species (ROS) in

4、 a dose-dependent manner inboth cell lines. Moreover, Western blotting shows that the levels of-H2AX are significantly elevated whencancer cells are treated with Artesunate in the higher dose range for 24 h. Artesunate also shows a time-dependent effect on the level of RAD51 in A2780 and HO8910 cell

5、s. In two types of non-malignant cells,normal human fibroblasts and immortalized epithelial cells, FTE-187, the level of RAD51 is not altered byArtesunate. In A2780 cells, the level of RAD51 mRNA is indeed decreased by the addition of Artesunate, in adose-dependent manner. Correspondingly, the promo

6、ter activity of RAD51 is significantly inhibited byArtesunate. In contrast, the RAD51 mRNA level in H8910 cells is not affected by Artesunate 3.體內(nèi)研究 Tumor growth is significantly reduced in the group receiving combined treatment of Artesunate and cisplatin(P 3.PROTOCOLKinase Assay 3 After treatment

7、with Artesunate for 24 h, cells are harvested and lysed in 1cell lysis buffer. Total proteins of15 to 25 g are separated by SDSand transferred to polyvinylidenedifluoride (PVDF) membranes.Membranes are blocked with 5% non-fat milk for 1 to 2 h at room temperature and then probed with primaryantibodi

8、es and incubated at 4C overnight. After extensive washing with TBS-T, membranes are incubatedwith appropriate HRP-conjugated secondary antibody for 1 h at room temperature, and then are detected byWestern ECL-enhanced luminol reagent 3.MCE has not independently confirmed the accuracy of these method

9、s. They are for reference only.Cell Assay 3 A2780 and HO8910 cells are cultured in RPMI 1640, Normal human fibroblasts (NHF) in DMEM, and FTE-187 in M199, supplemented with 10% fetal bovine serum, 100 units/mL penicillin, and 100 mg/mLstreptomycin. All the cells are incubated in a humidified atmosph

10、ere of 95% air and 5% CO2. Artesunate isapplied to the cultured cells at the concentration of 0, 5, 10, 25, or 50 g/mL for various periods. The reactiveoxygen species (ROS) production following Artesunate treatment is determined. Briefly, cells are loaded with5 M of CM-H2DCFDA and incubated at 37C f

11、or 20 min after treatment with Artesunate. Cells areresuspended using preserving fluid and analyzed with a FACSCanto II. The peak excitation wavelength foroxidized CM-H2DCFDA is 490 nm and emission is 530 nm 3.MCE has not independently confirmed the accuracy of these methods. They are for reference

12、only.Animal Four to six weeks old female athymic nude mice (BALB/c, nu/nu) are used. A2780 and HO8910 cells are2/3 Master of Small Molecules 您邊的抑制劑師www.MedChemEAdministration 3 harvested and resuspended in 0.1 ml of PBS, 5106 cells/0.2 mL are injected subcutaneously into the leftinguinal area of the

13、 mice. Two weeks later, mice bearing tumors (70 mm3 for A2780 and HO8910) arerandomly divided into 4 groups. Artesunate is administered daily via i.p. injection at doses of 50 mg/kg alonefor 16 days. The tumor growth is monitored every other day. Tumor volume is determined by the formula1/2ab2 where

14、 a is the long diameter (mm) and b is the short diameter (mm) 3.MCE has not independently confirmed the accuracy of these methods. They are for reference only.戶(hù)使本產(chǎn)品發(fā)表的科研獻(xiàn) Drug Des Dev Ther. 2019 Jul.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Ilamathi M, et al. Artesunate a

15、s an Anti-Cancer Agent Targets Stat-3 and Favorably Suppresses Hepatocellular Carcinoma. Curr TopMed Chem. 2016;16(22):2453-63.2. Lisewski AM, et al. Supergenomic network compression and the discovery of EXP1 as a glutathione transferase inhibited by artesunate.Cell. 2014 Aug 14;158(4):916-928.3. Wang B, et al. Artesunate sensitizes ovarian cancer cells to cisplatin by downregulating RAD51. Cancer B