Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEKRC-00715Cat.No.:HY-164411CASNo.:2079853-72-6分?式:C??H??F?N?O?分?量:542.51作?靶點:c-Met/HGFR作?通路:ProteinTyrosineKinase/RTK儲存?式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY?物活性KRC-00715?服有效的c-Met的抑制劑(IC50為9.0nM)，具有?度選擇性。KRC-00715在胃癌細(xì)胞中通過誘導(dǎo)G1/S阻滯來特異性抑制c-Met?表達(dá)細(xì)胞系的?長，降低了下游信號包括Akt和Erk以及c-Met活性。KRC-00715在胃癌細(xì)胞系Hs746中的細(xì)胞毒性IC50為39nM，且只抑制?表達(dá)c-Met細(xì)胞系的增殖。KRC-00715減?Hs746T異種移植??模型的腫瘤??[1]。體外研究KRC-00715exhibitsacytotoxicIC50of39nM,demonstratingitsefficacyasapotentc-Metinhibitor[1].KRC-00715(8,40,200,1000nM;3h;Hs746T,AGS)inhibitstheautophosphorylationofc-Met,indicatingthatthesuppressionofc-MetactivitysignificantlycontributestotheinhibitionofHs746Tcellproliferation[1].KRC-00715playsaroleinc-Methigh-expressioncelllinesandhasanIC50valueof39nMinHS746Tcells,andinhibitsc-Metautophosphorylationinhigh-expressioncelllines;phosphorylationofAKTandERK[1].KRC-00715(30nMand300nM)blockedSNU-5G1/SmorethanSNU-1,withnumericalvaluesof72.53and64.54at30nM,respectively,at300nM,thevaluesare73.62and83.64respectively[1].CellCytotoxicityAssay[1]CellLine:Hs746TConcentration:IncubationTime:3daysResult:ShowedthecytotoxicIC50ofHS746celllinewas39nm.CellCytotoxicityAssay[1]1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemECellLine:SNU-1,SNU-5,SNU-16,SNU-216,SNU-484,SNU-601,SNU-620,SNU-638,SNU-668,MKN-1,MKN-28,MKN-74,NCI-N87,KATOⅢ,AGS,SNU-719,MKN-45,Hs746TConcentration:0.0001-1μMIncubationTime:72hResult:ShowedtheIC50valuewaslessthanorequalto10nMinc-Metoverexpressingcelllinesandnotoxiceffectinlow-expressioncelllines.WesternBlotAnalysis[1]CellLine:Hs746T,SNU-638,SNU-620,AGS,SNU-1,MKN-1Concentration:8,40,200,1000nMIncubationTime:3hResult:Inhibitedc-Metautophosphorylationby70%,inhibitedtheproliferationofHS746Tcells,andinhibitedthephosphorylationofAktandERKinoverexpressedcelllines,withlowexpressionunaffected.CellCycleAnalysis[1]CellLine:SNU1,SNU5Concentration:30nM,300nMIncubationTime:24hResult:InducedSNU5arrestinG1/SphaseandnocellcyclearrestwasfoundinSNU1.InducedG1/Sarrestofc-metoverexpressingcellstoinhibitcellproliferation.體內(nèi)研究KRC-00715(50mg/kg;p.o.;oncedaily;10days)inhibitedtumorvolumeincreasedinanudemousexenograftHS746Tmodel[1].AnimalModel:NudemouseHs746Txenograftmodel[1].Dosage:50mg/kgAdministration:oralgavage(p.o.)；oncedaily;10daysResult:Reducedthetumorvolume,andtheweightofmicedidnotreduce.REFERENCES2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE[1].ChiHoonPark,etal.Novelc-Metinhibitorsuppressesthegrowthofc-Met-addictedgastriccancercells.BMCCancer.2016Jan22:16:35.McePdfHeightCaution:Producthasnotbeenfullyvalidatedfor