PROTAC-EML4-ALK-Degrader-1-Pro-BA-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors • ScreeningLibraries • Proteinswww.MedChemEPROTACEML4-ALKDegrader-1Cat.No.:HY-174368Synonyms:Pro-BA分子式:C₂₈H₃₅ClN₇O₃P分子量:584.05作用靶点:PROTACs;Apoptosis;Anaplasticlymphomakinase(ALK)作用通路:PROTAC;Apoptosis;ProteinTyrosineKinase/RTK储存方式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY生物活性PROTACEML4-ALKDegrader-2(Pro-BA)是一种具有选择性和口服有效的无连接子的EML4-ALKPROTAC降解剂，在H1322细胞中的DC50为74nM，T1/2为8h。PROTACEML4-ALKDegrader-2依赖于GID4和蛋白酶体途径促进靶蛋白的泛素化，导致细胞凋亡apoptosis。PROTACEML4-ALKDegrader-2可用于癌症的研究。(粉色:EML4-ALK配体(HY-40114);蓝色:GID4配体(HY-150908))[1]体外研究PROTACEML4-ALKDegrader-2(CompoundPro-BA)(0-1μM;0-24h)cansignificantlyandselectivelydegradethelevelsofEML4-ALKinH3122(DC50=74nM),BaF3-EML4-ALK(DC50=125nM)andneuroblastomaSK-N-BE(2)cells(DC50=2.1μM)[1].PROTACEML4-ALKDegrader-2(500nM;24h)increasestheproportionofG1phasecellsandsignificantlyincreasescellapoptosisinH3122cells[1].PROTACEML4-ALKDegrader-2(500nM;24h)inducesthedegradationofEML4-ALKthroughtheubiquitin-proteasomesysteminHEK293Tcells.[1].CellCycleAnalysis[1]CellLine:H3122cellsConcentration:500nMIncubationTime:24hResult:IncreasedtheproportionofG1phasecells.CellViabilityAssay[1]1/3 MasterofBioactiveMolecules—您身边的抑制剂大师www.MedChemECellLine:H3122cellsConcentration:0-1μMIncubationTime:48hResult:SignificantlyinhibitedthegrowthofH3122cells(IC50=34nM).ApoptosisAnalysis[1]CellLine:H3122cellsConcentration:500nMIncubationTime:24hResult:Significantlyincreasedtheproportionofearlyandlateapoptosis.体内研究PROTACEML4-ALKDegrader-2(CompoundPro-BA)(10mg/kg;i.p.;everyotherday;atotalof8doses)significantlyreducesthelevelofEML4-ALKandinhibitstumorgrowthinthefemalenudemicewithH3122xenografttumors[1].PROTACEML4-ALKDegrader-2(25mg/kg;p.o.;everytwodays;atotalof8doses)reducesthelevelofEML4-ALKandinhibitstumorgrowth,andexhibitslowtoxicityinthefemalenudemicewithH3122xenografttumors[1].AnimalModel:1×107H3122cellsinjectedfemalenudemice(4weeks)[1]Dosage:10mg/kgAdministration:Intraperitonealinjection(i.p.);everyotherdayforatotalof8dosesResult:SignificantlyreducedthelevelofEML4-ALKproteinintumors.Hadgoodtoleranceandnosignificantchangeinweight.Significantlyinhibitsthevolumeoftumors.AnimalModel:1×107H3122cellsinjectedfemalenudemice(4weeks)[1]Dosage:25mg/kgAdministration:Oraladministration(p.o.);everytwodaysforatotalof8dosesResult:SignificantlyreducedthelevelofEML4-ALKproteinintumors.Significantlyinhibitsthevolumeoftumors.Didnotchangethestructureinthemainorgans.REFERENCES2/3 MasterofBioactiveMolecules—您身边的抑制剂大师www.MedChemE[1].ZhangJ,etal.Linker-freePROTACsefficientlyinducethedegradationofoncoproteins.NatCommun.2025May23;16(1):4794.McePdfHeightCaution:Producthasnotbeenfullyvalidatedfor