UNBS5162 - CXCR Antagonist - 生命科學(xué)試劑 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEUNBS5162Cat. No.: HY-16509CAS No.: 956590-23-1分式: CHNO分量: 326.35作靶點(diǎn): CXCR; Autophagy作通路: GPCR/G Protein; Immunology/Inflammation; 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 : 21

2、.5 mg/mL (65.88 mM; Need ultrasonic and warming)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液1 mM 3.0642 mL 15.3210 mL 30.6419 mL5 mM 0.6128 mL 3.0642 mL 6.1284 mL10 mM 0.3064 mL 1.5321 mL 3.0642 mL請(qǐng)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(chǔ)備液，并請(qǐng)注意儲(chǔ)備液的保存式和期限。BIOLOGICAL ACTIVITY物活性 UNBS5162種譜的趨化因配體 CXCL 拮抗劑，具有抗腫瘤活性。

3、IC50 & Target CXCL體外研究UNBS5162 is a pan-antagonist of CXCL chemokine expression and exhibits weak antiproliferative activityagainst human cancer cell lines with mean IC50 of 17.9 M. UNBS5162 markedly impairs PC-3 tumor cellgrowth kinetics, without inducing senescence, whereas the reverse feature is

4、observed with respect to DU-1/3 Master of Small Molecules 您邊的抑制劑師www.MedChemE145 cells 1. UNBS5162 is cytotoxic to a range of human cancer cell lines including glioblastoma (Hs683 andU373MG), colorectal (HCT-15 and LoVo), non-small-cell lung (A549) and breast (MCF-7), with IC50s of 0.5-5M. UNBS5162

5、also markedly increases the levels of expression of LC3-I and LC3-II in human cancer cells.UNBS5162 displays no anti-topoisomerase II activity. Moreover, UNBS5162 induces cancer cell deaththrough lysosomal membrane permeabilization (LMP) in PC3 prostate cancer cells but not in U373glioblastoma cells

6、, with this LMP process occurring as an UNBS5162-induced decrease in Hsp70 expression2. UNBS5162 inhibits the proliferation of esophageal cancer squamous cells via the PI3K/AKT signalingpathway. UNBS5162 downregulates the protein expression of proteins associated with the PI3K/AKTsignaling pathway,

7、including the levels of phosphorylated (p)-AKT, p-mechanistic target of rapamycin kinase,ribosomal protein S6 kinase 1 and cyclin D1 3.體內(nèi)研究 UNBS5162 (20 mg/kg, i.v.) increases the therapeutic benefits of taxol in vivo in the orthotopic human PC-3prostate cancer model 1.PROTOCOLAnimal Mice 1Administr

8、ation 1 Orthotopic xenografts are obtained by injecting 2.5 106 human PC-3 or DU-145 cells into the prostate of 6-week-old male nu/nu mice (n = 9 animals per treatment group). All grafts are performed under anesthesiasaline/Rompun/Imalgene; 5:1:1 by volume. The end point in these orthotopic experime

9、nts is the survivalperiod of the tumor-bearing mice after the administration of UNBS3157, UNBS5162, or reference anticanceragents (taxol, mitoxantrone, and amonafide). However, for ethical reasons, animals are killed when 20% ofbody weight have been lost compared to that determined at the time of tu

10、mor grafting. All animals areweighed three times a week. Autopsies and histologic diagnoses are performed on each mouse to confirmthe presence of tumor development; 100% is achieved. In the case of UNBS5162 experiments in the PC-3model, after the sacrifice of animals, tumors are removed from both dr

11、ug-treated 10 mg/kg, intravenous(i.v.) and vehicle-treated mice, fixed in buffered formalin, embedded in paraffin, and 5-m-thick sectionstaken. These histologic slides are then stained with hematoxylin and eosin for blood vessel counts 1.MCE has not independently confirmed the accuracy of these meth

12、ods. They are for reference only.戶使本產(chǎn)品發(fā)表的科研獻(xiàn) Onco Targets Ther. 2017 Nov 6;10:5303-5309. Thorac Cancer. 2018 Jan;9(1):105-111. Drug Dev Ind Pharm. 2019 Apr 17:1-17. Cancer Manag Res. 2019 Mar 22;11:2339-2348. Mol Med Rep. 2018 Jan;17(1):549-555.See more customer validations on HYPERLINK / www.MedChe

13、mEREFERENCES2/3 Master of Small Molecules 您邊的抑制劑師www.MedChemE1. Mijatovic T, et al. UNBS5162, a novel naphthalimide that decreases CXCL chemokine expression in experimental prostate cancers.Neoplasia. 2008 Jun;10(6):573-86.2. Tina Mahieu, et al. UNBS5162: A novel naphthalimide derivative with potent pro-autophagic effects in human cancer cells. CancerResearch, 2007 May; 67(9) Supplement.3. He D, et al. UNBS5162 inhibits the proliferation of esophageal cancer squamous cells via the PI3K/AKT signaling pathway. Mol MedRep. 2018 Jan;17(1):54