MKT-077-FJ-776-DataSheet-生命科學試劑-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEMKT-077Cat. No.: HY-15096CAS No.: 147366-41-4Synonyms: FJ-776分式: CHClNOS分量: 432作靶點: HSP作通路: Cell Cycle/DNA Damage; Metabolic Enzyme/Protease儲存式: Powder -20C 3 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實驗 DMSO : 41.67 mg/mL

2、 (96.46 mM; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 2.3148 mL 11.5741 mL 23.1481 mL5 mM 0.4630 mL 2.3148 mL 4.6296 mL10 mM 0.2315 mL 1.1574 mL 2.3148 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存式和期限。體內(nèi)實驗 請根據(jù)您的實驗動物和給藥式選擇適當?shù)娜芙獍福渲魄罢埾扰渲瞥吻宓膬湟?，再依次添加助溶?為保證實驗結果的可靠性，體內(nèi)實驗的作液，建議您現(xiàn)現(xiàn)配，

3、當天使；澄清的儲備液可以根據(jù)儲存條件，適當保存；以下溶劑前的百分 指該溶劑在您配制終溶液中的體積占)：1. 請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.08 mg/mL (4.81 mM); Clear solution2. 請依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.08 mg/mL (4.81 mM); Clear solution1/3 Master of Small Molecules 您邊的抑制劑師www.MedChemEBIOLOGICAL AC

4、TIVITY物活性 MKT-077種花菁染料，也 種熱休克蛋 70 (Hsp70) 抑制劑，且具有顯著的抗腫瘤活性。IC50 & Target HSP70體外研究 MKT-077 is a rhodacyanine dye and also a heat shock protein 70 (Hsp70) inhibitor which exhibits significantantitumor activity. MKT-077 treatment (0.1 to 10 M dose ranges) for 48 hours can effectively decrease TTcell vi

5、ability. MKT-077 treatment results in accumulation of cells in the G0/G1 phase in a dose-dependentmanner, and also increases sub-G0/G1 phase population in TT cell culture in a dose-dependent manner.MKT-077 also downregulates cellular levels of the proliferation marker, Ki67, and the S-phase transcri

6、ptionfactor, E2F-1, in TT and MZ-CRC-1 cells. Moreover, flow cytometry using different doses of MKT-077reveales that TT cells can uptake and retain MKT-077 at significantly higher levels than MZ-CRC-1 cells 1.MKT-077 has EC50 values of 1.40.2 and 2.20.2 M against MDA-MB-231 and MCF7 breast cancer ce

7、lls,respectivelyl 2.體內(nèi)研究 Systemic administration of MKT-077 significantly delays the growth of TT xenografts in mice throughout thetreatment. At the end of MKT-077 treatment, it is found that tumor weights are about two-times less in MKT-077-treated group than in control group. MKT-077 treatment als

8、o results in weight loss and general toxicity inanimals 1. Results show that the succinate-induced, ADP-stimulated respiratory rate in mitochondriaisolated from the liver of rats treated with a bolus i.v. injection of 15 mg MKT-077 1kg body weight each dayfor 5 days is significantly lower than that

9、of untreated controls 3.PROTOCOLCell Assay 1 Cells are incubated with 1 M MKT-077 and 100 nM Mitotracker Green FM in culture medium for 30 minutesat 37C in the dark, washed with PBS, switched into phenol-red free medium before visualizing fluorescenceunder a microscope. Pictures are acquired and pro

10、cessed with software. For flow cytometric measurement,MKT-077-treated cells are resuspended in 0.1% bovine serum albumin/PBS and analyzed by flow cytometry.Data from 20,000 cells are analyzed using FCS Express software 1.MCE has not independently confirmed the accuracy of these methods. They are for

11、 reference only.Animal The 1107 TT cells in 200 L Hanks balanced salt solution are inoculated subcutaneously into the rearAdministration 1 flanks of 6-week-old female athymic nude (nu/nu) mice. Once palpable, tumors are measured using calipersat intervals indicated in the text. When tumor volume rea

12、ches 100 mm3, mice are sorted into groups of 8 toachieve equal distribution of tumor size in all treatment groups. Group 1 receives only the vehicle (1:9mixture of DMSO/saline) and group 2 receives MKT-077 (10 mg/kg body weight/dose). A 200 L of ethersolution is administered by intraperitoneal injec

13、tion every 2 days (total 10 doses). At the end of theexperiments, animals are euthanized by CO2 asphyxiation 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES2/3 Master of Small Molecules 您邊的抑制劑師www.MedChemE1. Starenki D, et al. Selective Mit

14、ochondrial Uptake of MKT-077 Can Suppress Medullary Thyroid Carcinoma Cell Survival In Vitro and InVivo. Endocrinol Metab (Seoul). 2015 Dec;30(4):593-603.2. Li X, et al. Analogs of the Allosteric Heat Shock Protein 70 (Hsp70) Inhibitor, MKT-077, as Anti-Cancer Agents. ACS Med Chem Lett.2013 Nov 14;4(11).3. Weisberg EL, et al. In vivo administration of MKT-077 causes partial yet reversible impairment of mitochondrial function. Cancer Res.1996 Fe