BRAFV600E-ABL2-IN-1-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEBRAFV600E/ABL2-IN-1Cat.No.:HY-178382分⼦式:C₂₄H₂₀BrClN₄O₃S分⼦量:559.86作⽤靶点:Raf;Bcr-Abl;P-glycoprotein;PERK;Apoptosis作⽤通路:MAPK/ERKPathway;ProteinTyrosineKinase/RTK;MembraneTransporter/IonChannel;CellCycle/DNADamage;Apoptosis储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY⽣物活性BRAFV600E/ABL2-IN-1⼀种BRAFV600E(IC50=0.088μM)/ABL2(IC50=0.3μM)双重抑制剂。BRAFV600E/ABL2-IN-1可降低P-糖蛋⽩的表达。BRAFV600E/ABL2-IN-1可有效抑制A375-R⿊⾊素瘤细胞中的p-CrkL(Abl2信号通路)和p-ERK1/2(BRAFV600E通路)。BRAFV600E/ABL2-IN-1可导致细胞周期停滞于G1期，从⽽抑制细胞进⼊S期及后续各期以及G2/M期。BRAFV600E/ABL2-IN-1显著增加晚期凋亡(apotosis)细胞的⽐例。BRAFV600E/ABL2-IN-1可⽤于⿊⾊素瘤的研究[1]。IC50&TargetBRafV600EBRafV600E0.088μM(IC50)0.088μM(IC50)体外研究BRAFV600E/ABL2-IN-1(Compound8h)(0.01-100μM,48h)exhibitsthebestactivitytowardsSK-MEL5cellsatthemelanomapanel,withaGI50of0.54μM,demonstratingmarkedcytostaticactivityagainstmelanoma(SK-MEL-5;TGI=19.95μM)andcoloncancer(HT29;TGI=26.30μM)[1].BRAFV600E/ABL2-IN-1(0.125-1μM,72h)significantlydownregulatesP-gpexpressioninSK-MEL-5cells[1].BRAFV600E/ABL2-IN-1(0.4-100μM)demonstratesIC50valuesof6.888μg/mL(~12.3μM)inA375cells(BRAFV600Emutant)and11.242μg/mL(~20.1μM)inA375-Rcells(vemurafenib-resistant),and28.776μMinWI-38cells[1].BRAFV600E/ABL2-IN-1significantlyreducesthephosphorylationlevelsofp-CrkL(downstreamofABL2)andp-ERK1/2(downstreamofBRAF),whiletotalproteinremainsunchanged.p-CrkLdecreasesby67.7%,andp-ERK1/2decreasesby63.0%inA375-Rcells[1].BRAFV600E/ABL2-IN-1(0.54μM,48h)inhibitscellproliferationinSK-MEL-5cellsbyinducingG1phasearrestandapoptosis[1].1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemERealTimeqPCR[1]CellLine:SK-MEL-5cellsConcentration:0.125μM,0.25μM,0.5μM,1μMIncubationTime:72hResult:Showedapproximately67.4%downregulationofP-gpexpressioninSK-MEL-5cells.CellCycleAnalysis[1]CellLine:SK-MEL-5cellsConcentration:0.54μMIncubationTime:48hResult:CausedG0-G1phasearrest(58.12%vs.control44.63%),andreducedSandG2/Mphases.ApoptosisAnalysis[1]CellLine:SK-MEL-5cellsConcentration:0.54μMIncubationTime:48hResult:Increasedearlyapoptosis(25.61%vs.control0.33%)andlateapoptosis(13.89%vs.control0.15%).REFERENCES[1].BadawyMAS,etal.Targetingmelanomaresistance:Noveloxindoleandnon-oxindole-basedbenzimidazolederivativesaspotentdualinhibitorsofBRAFV600EandABL2kinases.EurJMedChem.2025Dec15;300:118096.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplic