NSC305787 - Ezrin 抑制剂 - 生命科学试剂 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemENSC305787Cat. No.: HY-18931CAS No.: 785718-37-8分式: CHClNO分量: 445.42作靶点: Others作通路: Others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 : 6 mg/mL (13.47 mM; Need ultrasonic and warming)Mass

2、Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.2451 mL 11.2254 mL 22.4507 mL5 mM 0.4490 mL 2.2451 mL 4.4901 mL10 mM 0.2245 mL 1.1225 mL 2.2451 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。体内实验 请根据您的实验动物和给药式选择适当的溶解案，配制前请先配制澄清的储备液，再依次添加助溶剂(为保证实验结果的可靠性，体内实验的作液，建议您现现配，当天使；澄清的储备液可以根据储存条件，适当保存；以下溶剂前的百分

3、指该溶剂在您配制终溶液中的体积占)：1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 0.6 mg/mL (1.35 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 0.6 mg/mL (1.35 mM); Clear solution3. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 0.6 mg/mL (1.35 mM); Clear solution1

4、/3 Master of Small Molecules 您边的抑制剂师www.MedChemEBIOLOGICAL ACTIVITY物活性 NSC305787种 ezrin 抑制剂，Kd 值为 5.85 M，抑制 PKC 导致的 ezrin 磷酸化，IC50 of 8.3 M，具有抗肿瘤活性。IC50 & Target Kd: 5.85 M (ezrin) 1IC50: 8.3 M (ezrin) 1体外研究 NSC305787 is an inhibitor of ezrin with a Kd of 5.85 M, and has antitumor activity. NSC30578

5、7 inhibits PKC phosphorylation of Ezrin, Moesin, Radixin, MBP, with IC50s of 8.3, 9.4, 55, 58.9 M, respectively.NSC305787 binds to PKC with a Kd value of 172.4 M, and inhibits ezrin T567 phosphorylation primarily viaits binding to ezrin and not through inhibition of PKC kinase activity. NSC305787 (1

6、, 10 M) shows inhibitoryactivity against ezrin-mediated invasion of K7M2 osteosarcoma (OS) cells. Moreover, NSC305787 (10 M)reduces cell motility phenotypes in zebrafish and blocks OS metastatic growth in lung organ culture 1.体内研究 NSC305787 (0.240 mg/kg/day, i.p.) suppresses ezrin-dependent osteosar

7、coma metastatic growth in mouselung 1. NSC305787 (240 g/kg, i.p.) dramatically inhibits pulmonary metastasis in a transgenic mousemodel of osteosarcoma (Osx-Cre+p53fl/flpRBfl/fl) and shows a more favorable pharmacokinetic profilecompared with NSC668394 in the mouse model 2.PROTOCOLCell Assay 1 Human

8、 umbilical vein endothelial cells (HUVECs; 2.5 104/well) are seeded in a 96-well plate in endothelialgrowth media-2. Following formation of a confluent HUVEC monolayer (-32 h), endothelial growth media-2 isaspirated and a layer of osteosarcoma (OS) cells (1.0 104 cells/well) is added to Dulbeccos mo

9、dified Eaglemedium containing NSC305787. This specific time point is accepted as 0 h of treatment, and invasion ismonitored during the subsequent 5 h by measuring changes in resistance at the cell-electrode interphase.The cell index is calculated according to the following formula: cell index = (Rt

10、R0)/F, where Rt is resistanceat time point t, R0 is background resistance (measured with media alone, no cells) and F is frequency atwhich the measurement is taken (10 kHz) 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Mice 2Administration 2

11、The Osx-Cre+p53fl/flpRBfl/fl transgenic mouse model of osteosarcoma is used in the assay. Mice are treatedwith 240 g/kg/day NSC305787, 226 g/kg/day NSC668394, or vehicle (DMSO, 1%) once daily, five times aweek by i.p. injection in a volume of 100 L. At the end of the study, lung and tumor samples ar

12、e isolatedupon necropsy. Half of each sample is flash frozen immediately in liquid nitrogen, and the other half is fixedin 10% formalin for 18-24 h, transferred to 70% ethanol, and stored at room temperature 2.MCE has not independently confirmed the accuracy of these methods. They are for reference

13、only.户使本产品发表的科研献2/3 Master of Small Molecules 您边的抑制剂师www.MedChemE PLoS Pathog. 2019 May 9;15(5):e1007737.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Bulut G, et al. Small molecule inhibitors of ezrin inhibit the invasive phenotype of osteosarcoma cells. Oncogene. 2012 Jan19;31(3):269-81.2. elik H, et al. Ezrin Inhibition Up-regulates Stress Response Gene Expression. J Biol Chem. 2016 Jun 17;291(25):13257-70.