Adjudin-AF-2364-DataSheet-生命科學試劑-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEAdjudinCat. No.: HY-18996CAS No.: 252025-52-8Synonyms: AF-2364分式: CHClNO分量: 335.19作靶點: Chloride Channel; Mitochondrial Metabolism作通路: Membrane Transporter/Ion Channel; MetabolicEnzyme/Protease儲存式: Powder -20C 3 years4C 2 yearsIn

2、 solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實驗 DMSO : 34 mg/mL (101.44 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 2.9834 mL 14.9169 mL 29.8338 mL5 mM 0.5967 mL 2.9834 mL 5.9668 mL10 mM 0.2983 mL 1.4917 mL 2.9834 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，并請注意儲備液的保

3、存式和期限。BIOLOGICAL ACTIVITY物活性 Adjudin種泛研究的男性避孕試劑，具有優(yōu)越的線粒體抑制作。 Adjudin 也 種有效的 Cl- 通道阻斷劑。IC50 & Target Cl- channel 11/3 Master of Small Molecules 您邊的抑制劑師www.MedChemEMitochondria 2體外研究 Adjudin is a potent blocker of Cl- channels: disrupting Cl- ion transport function results in a decline in spermcapacit

4、ation and fertilizing ability in humans in vitro 1. Adjudin (ADD) is a mitochondria inhibitor 2. Adjudinis a molecule that mediates adherens junction disruption at the Sertoli-germ cell interface. To investigate theeffect of Adjudin on cancer cells, more than ten different types of human or mice can

5、cer cell lines are treatedwith increasing concentrations of Adjudin and the cell proliferation is measured by the modified MTT assay.Adjudin inhibits cell proliferation in a dose dependent manner in SGC-7901 (human gastric adenocarcinomacell), MDA-MB-231 (human breast adenocarcinoma cell), Smmc-7721

6、 (human hepatoma cell) and MIA Paca-2 (human pancreatic adenocarcinoma cell) cells. The IC50 of Adjudin is determined to be 58.0 M, 13.8 M,72.3 M and 52.7 M against SGC-7901, MDA-MB-231, Smmc-7721 and MIA Paca-2 cells, respectively,after treatment for 24 h. Similar results are obtained in other huma

7、n and mice cancer cell lines. The IC50 ofAdjudin in A549 cells and PC3 cells is 63.1 M and 93.0 M, respectively. For WI-38 and BPH-1 cells, theIC50 of Adjudin can be observed at more than 300 M and 200 M, respectively, which is about 5 times and2 times more than that for the cancer cell lines A549 a

8、nd PC3 3.體內(nèi)研究 To determine whether Adjudin can inhibit lung and prostate cancer growth in vivo, the effect of Adjudin istested in a subcutaneous model of lung and prostate cancer. Human lung carcinoma cells A549 and prostatecarcinoma cells PC3 are injected into athymic nude mice subdermally at the l

9、ower back site respectively.Mice are then randomized into two treatment groups with similar mean tumor sizes: Adjudin and vehicle(control). Approximately 2 weeks after tumor inoculation Adjudin is injected intraperitoneally once every threedays in lung carcinoma cells and every other day in prostate

10、 carcinoma cells at 100 mg/kg. Adjudin treatmentcan be well tolerated in rodent. And Adjudin-treated mice show significant tumor growth inhibition comparedwith the control group (P 3.PROTOCOLCell Assay 3 A549 cells, WI-38 cells, BPH-1 cells, PC-12 cells and other cell lines are seeded in 96-well pla

11、tes at thedensity of 0.5104/well in the complete growth medium and incubated for 24 h. Then the growth medium isreplaced with a serial dilution of Adjudin (300 M, 100 M, 30 M, 10 M, 3 M and 0) in growth medium(without serum). The cells are incubated for another 24 h followed by the addition of 10 l

12、of Cell CountingKit-8 solution to each well. After 4 h of incubation at 37 C in the cell incubator, the absorbance at 450 nm ismeasured using a microplate reader 3.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Mice 3Administration 3 The male BA

13、LB/C nude mice weighing 20g are equally implanted with A549 cells (0.5107 cells) containing3 mg/mL of matrigel and PC3 cells (1106 cells) hypodermically. After 2 weeks, the mice with palpabletumors are divided into two groups (n=4 per group in each experiment and repeated with a total of threeexperi

14、ments): i.p. injection of Adjudin which is dissolved in corn oil from a DMSO stock solution with finaladministered quantity at 100 mg/kg (300 M used in vitro); the equivalent vehicle control group areadministered with the same amount of corn oil and DMSO via i.p. injection. Adjudin or vehicles aread

15、ministered every three day in A549 and every other day in PC3 up to 2 weeks. Tumor volumes are2/3 Master of Small Molecules 您邊的抑制劑師www.MedChemEdetermined and calculated.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Li K, et al. Inhibition

16、 of sperm capacitation and fertilizing capacity by adjudin is mediated by chloride and its channels in humans. HumReprod. 2013 Jan;28(1):47-59.2. Li X, et al. Combination delivery of Adjudin and Doxorubicin via integrating drug conjugation and nanocarrier approaches for thetreatment of drug-resistant cancer cells. J Mater Chem B. 2015 Feb 28;3(8):1556-1564.3. Xie QR, et al. Male contraceptive Adjudin is a potential anti-cancer dr