GW2974-DataSheet-生命科學(xué)試劑-MCE

Hotline:400-820-3792Inhibitors ? ScreeningLibraries ? Proteinswww.MedChemEGW2974Cat.No.:HY-112293CASNo.:202272-68-2分子式:C??H??N?分子量:395.46作用靶點(diǎn):EGFR作用通路:JAK/STATSignaling;ProteinTyrosineKinase/RTK儲(chǔ)存方式: 4°C,sealedstorage,awayfrommoistureInsolvent:-80°C,6months;-20°C,1month(sealedstorage,awayfrommoisture)BIOLOGICALACTIVITY生物活性GW2974是一種強(qiáng)效的EGFR和HER2雙抑制劑，其IC50值分別為0.007μM和0.016μM。GW2974對(duì)EGFR和HER2的結(jié)構(gòu)域具有體外抑制作用，并抑制腫瘤細(xì)胞的生長(zhǎng)，可用于膠質(zhì)母細(xì)胞瘤(GBM)疾病的研究。IC50&TargetEGFRL858R/T790MHER20.007μM(IC50)0.016μM(IC50)體外研究GW2974(0.5-50μM,3h)hasanobviouscytotoxicityappearedat10μMoraboveandinhibitscellproliferationofU87MGandU251MGcellsat0.5-5μMafter24htreatment[1].GW2974(0.5-5μM,24h)hasadose-relatedroleinGBMcellinvasionandmigration[1].GW2974(0.001-100μM,24h)inhibitsBT474,HN5,N87cellsgrowth[2].CellViabilityAssay[1]CellLine:U87MG,U251MGConcentration:0.5-50μMIncubationTime:3hResult:ReducedU87MGandU251MGcellsviabilityto89.4%and86.3%in0.5μMand5μMcomparedwithcontrol.CellProliferationAssay[1]1/3 MasterofBioactiveMolecules—您身邊的抑制劑大師www.MedChemECellLine:U87MG,U251MGConcentration:0.5-5μMIncubationTime:24hResult:InhibitedU87MGandU251MGcellsproliferationin0.5μMand5μM.CellInvasionAssay[1]CellLine:U87MG,U251MGConcentration:0.5-5μMIncubationTime:24hResult:Reducedthepercentageto55.6%and48.6%ofU87MGandU251MGcellsin0.5μM,respectively.CellMigrationAssay[1]CellLine:U87MG,U251MGConcentration:0.5-5μMIncubationTime:24hResult:Decreasedtherelativemigrationdistances(percentage)ofU87MGandU251MGcellsto40.2%and51.6%in0.5μM,respectively.ResultedinarelativemigrationdistancesofU87MGandU251MGcellsin5μMcomparedwithcontrol.CellProliferationAssay[2]CellLine:BT474,HN5,N87Concentration:0.001-100μMIncubationTime:24hResult:Inhibitedcellgrowthby50%atconcentrations>1.0μMwithIC50s<0.4μM.體內(nèi)研究GW2974(30mg/kg,100mg/kgforOralgavage,onceaday)inhibitsGBMgrowth,invasion,andangiogenesisindoseof30mg/kgbutabrogatedtheinhibitoryeffectoflow-doseGW2974ontumorinvasionindoseof100mg/kginGBMxenograftmicemodel[1].GW2974(10mg/kg,30mg/kg,Oralgavage,twiceaday)inhibitsthegrowthoftumorinCD-1nudemice(HN5)andC.B-17SCIDmice(BT474)modelsinadoseddependentmanner[2].2/3 MasterofBioactiveMolecules—您身邊的抑制劑大師www.MedChemEAnimalModel:GBMxenograftmicemodel[1]Dosage:30mg/kg,100mg/kgAdministration:Oralgavage(p.o.)Result:Deceleratedtumorgrowthatdoseof30mg/kgand100mg/kg.Inhibitedtheinvasiontoperitumorareasoftumorsin30mg/kggroupbutaugmentedtumorinvasionin100mg/kggroupofbraintissues.Inhibitedangiogenesisindosesof30mg/kgand100mg/kg.AnimalModel:CD-1nudemice(HN5),C.B-17SCIDmice(BT474)[2]Dosage:10mg/kg,30mg/kgAdministration:Oralgavage(p.o.)Result:InhibitedtumorgrowthintheHN5modelbytreatmentdosewith30mg/kg.InhibitedtumorgrowthintheHN5modelabout95%inhibitionandBT474modelabout50%inhibitionbytreatmentdosewith10mg/kg.REFERENCESWangL,etal.Differentialeffectsoflow-andhigh-doseGW2974,adualepidermalgrowthfactorreceptorandHER2kinaseinhibitor,onglioblastomamultiformeinvasion.JNeurosciRes.2013Jan;91(1):128-37.RusnakDW,etal.Thecharacterizationofnovel,dualErbB-2/EGFR,tyrosinekinaseinhibitors:potentialtherapyforcancer.CancerRes.2001Oct1;61(19):7196-20.McePdfHeightCaution:Producthasn