PXB17-DataSheet-生命科學(xué)試劑-MCE

Hotline:400-820-3792Inhibitors ? ScreeningLibraries ? Proteinswww.MedChemEPXB17Cat.No.:HY-158050分子式: C??H??N?O?分子量: 545.63儲存方式: PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY生物活性PXB17可以通過阻斷PI3K/AKT/mTORC1信號的激活抑制CSF1R，口服有效，明顯抑制CRC的生長，提高PD-1mAb的療效并且減少CRC的腫瘤復(fù)發(fā)。(CSF1RIC50=1.7nM)體外研究PXB17(30-3000nM;4h)dose-dependentlycanincreasestabilityofCSF1R[1].PXB17(30,100nM;24h)haltscholesterolbiosynthesisandpreventCRCdevelopmentbyblockingPI3K-AKT-mTORC1signalingtoinduceconversionoftheM2phenotypetotheM1phenotype[1].PXB17(10,30,100nM;72h)blocksCRCcellgrowthbyenhancinganti-tumorimmunity[1].RealTimeqPCR[1]CellLine:BMDMsConcentration:10,30,100nMIncubationTime:24hResult:InducedconversionofTAMsfromM2toM1phenotypeintumortissuesofCRC.Immunofluorescence[1]CellLine:BMDMsConcentration:10,30,100nMIncubationTime:24h1/2 MasterofBioactiveMolecules—您身邊的抑制劑大師www.MedChemEResult:HaltedcholesterolbiosynthesisandfacilitatestheconversionofM2macrophagestoM1phenotypebyblockingCSF-1/CSF1RaxisandsubsequentPI3K-AKT-mTORC1signalingtransduction.體內(nèi)研究PXB17(C57BL/6micewereinoculatedwithMC-38cell;10,20mg/kg;p.o.;daily)effectivelyinhibitstumorgrowth[1].PXB17(C57BL/6,BALB/cmicewereinoculatedwithMC-38cell;20mg/kg;p.o.;daily)hasmacrophage-dependent.TheTGIwasstrongercomparedtothepositivecontrolPLX3397(HY-16749)attheequivalentdosage[1].PXB17(CT-26(MSS),MC-38(MSI-H)mice;20mg/kg;p.o.;daily)ConcomitantusewithPD-1mAbcanimproveanti-tumorefficacyandreducerecurrence[1].AnimalModel:micewereinoculatedwithMC-38cell[1]Dosage:10,20mg/kgAdministration:p.o.Result:Results:Mitigatedtumorprogression.20mg/kgdosageshowedstrongeranti-tumoreffectscomparedtoPLX3397(HY-16749).20mg/kgdosageenhancedTcell-drivenimmuneresponse.AnimalModel:micewereinoculatedwithCT-26cell[1]Dosage:20mg/kgAdministration:p.o.Result:Significantlyslowedtumorprogressionwithmacrophage-dependent.AnimalModel:micewereinoculatedwithHCT116cells[1]Dosage:10,20mg/kgAdministration:p.o.Result:Activatedsystemicanti-tumorimmuneresponses.REFERENCESQiLetal.CSF1Rinhibitionreprogramstumor-associatedmacrophagestopotentiateanti-PD-1therapyefficacyagainstcolorectalcancerPharmacologicalResearch202(2024)107126.McePdfHeight2/2 MasterofBioactiveMolecules—您身邊的抑制劑大師www.MedChemECaution:Producthasnotbeenfullyvalidatedformedicalapplications.For