SBI-183-生命科學(xué)試劑-MCE

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemESBI-183Cat.No.:HY-165245CASNo.:625403-59-0分?式:C??H??N?O?分?量:296.36作?靶點(diǎn):TransmembraneGlycoprotein作?通路:Immunology/Inflammation儲(chǔ)存?式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY?物活性SBI-183?種具有?服活性的QSOX1抑制劑(Kd:20μM)。SBI-183可抑制腎癌細(xì)胞系、三性乳腺癌細(xì)胞系、肺腺癌細(xì)胞系和胰腺導(dǎo)管腺癌的增殖和侵襲表型。SBI-183可體內(nèi)抑制兩種?腎細(xì)胞癌異種移植??模型的腫瘤?長[1]。體外研究SBI-183(6.25-50μM,15min)inhibitstheenzymaticactivityofrQSOX1inadose-dependentmanner[1].SBI-183inhibitsproliferationoftumorcells,butdoesnotkillfibroblastsorrapidlyproliferatingPBMC(0.625-20μmol/L,5days),inhibitsviabilityof786-O,RCJ-41T2,andMDA-MB-231withIC50sof4.6μM,3.9μM,and2.4μM,respectively(0.076nM-40μM,72h)[1].SBI-183(2.5-20μM,4-8days)inhibitstumorinvasioninboth2Dand3Dmodelsof786-O,RCJ-41T2,MDA-MB-231,A549andMIAPaCa2dose-dependently[1].CellProliferationAssay[1]CellLine:786-O,RCJ-41T2,MDA-MB-231,A549和MIAPaCa2Concentration:0.625,1.25,2.5,5,10,20μMIncubationTime:5daysResult:Inhibitedthegrowthofeachtumorcellinaconcentration-dependentmanner.CellInvasionAssay[1]CellLine:786-O,RCJ-41T2,MDA-MB-231,A549和MIAPaCa21/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEConcentration:2.5,5,10,20μMIncubationTime:4,6,8daysResult:ReducedinvasionthroughMatrigelineachcellline.體內(nèi)研究SBI-183(786-O:400μg/mouse/day,p.o.,35days;RCJ-41T2:100mg/kg,p.o.,21days)inhibitstumorgrowthintwoindependenthumanxenograftmousemodelsofrenalcellcarcinoma[1].AnimalModel:Humanxenograftmousemodelsofrenalcellcarcinoma(786-OandRCJ-41T2)[1]Dosage:400μg/mouse/day(786-O);100mg/kg(RCJ-41T2)Administration:Oralgavage(p.o.)Result:Inhibitedthegrowthof786-OandRCJ-41T2invivo.Reducedlaminin-α4depositioninRCJ-41T2mousexenografts.REFERENCES[1].Fifield,etal.MolecularInhibitorofQSOX1SuppressesTumorGrowthInVivo.Molecularcancertherapeutics.2020,19(1),112–122.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.