RSH-7-DataSheet-生命科學(xué)試劑-MCE

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemERSH-7Cat.No.:HY-151961CASNo.:2764609-97-2分?式:C??H??FN?O分?量:436.49作?靶點:Btk;FLT3作?通路:ProteinTyrosineKinase/RTK儲存?式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY?物活性RSH-7?種有效的BTK和FLT3抑制劑，IC50分別為47、12nM。RSH-7誘導(dǎo)細胞凋亡(apoptosis)并顯?抗增殖活性。RSH-7抑制BTK和FLT3信號轉(zhuǎn)導(dǎo)并顯?出抗腫瘤活性[1]。IC50&TargetIC50:47nM(BTK);12nM(FLT3)[1]體外研究RSH-7(1-1000nM;72h)showsantiproliferativeactivitieswithIC50sof17,3,11,930nMforJeko-1,MV-4-11,Molt4,K562cells,respectively[1].RSH-7(30,150,750nM;72h)decreasestheexpressionofp-BTK(TYR223),p-PLCγ(Tyr1217),p-FLT3(Tyr589),p-STAT5(TYR694)inadose-dependentmanner[1].RSH-7(30,150,750nM;72h)inducesapoptosisandincreasestheexpressionofBAX,p53,cleavedcaspase3inadosedependenmannerinjeko-1cells[1].CellViabilityAssay[1]CellLine:Jeko-1,MV-4-11,Molt4,K562cellsConcentration:1-1000nMIncubationTime:72hResult:ShowedantiproliferativeactivitieswithIC50sof17,3,11,930nMforJeko-1,MV-4-11,Molt4,K562cells,respectively.WesternBlotAnalysis[1]1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemECellLine:jeko-1cellsConcentration:30,150,750nMIncubationTime:72hResult:ReducedbothBTK,PLCγ2,FLT3andSTAT5phosphorylationinadose-dependentmanner.ApoptosisAnalysis[1]CellLine:jeko-1cellsConcentration:30,150,750nMIncubationTime:72hResult:Dose-dependentlyinducedcellapoptosisandupregulatedtheexpressionofpro-apoptoticproteinBAX,p53,cleavedcaspase3.體內(nèi)研究RSH-7(25,50mg/kg;i.p.;dailyfor16days)showsanti-tumoractivitywithsignificantlyanddose-dependentlysuppressesthetumorgrowthinmouse[1].AnimalModel:FemaleNOD/SCIDmice(jeko-1cell-inoculatedxenograftNOD/SCIDmicemodels)[1]Dosage:25,50mg/kgAdministration:I.p.;dailyfor16daysResult:Suppressedtumorgrowthinadose-dependentmanner,withtumorgrowthinhibition(TGI)valuesof66.95%and79.78%atdosesof25and50mg/kg,AnimalModel:FemaleNOD/SCIDmice(MV4-11cell-inoculatedxenograftNOD/SCIDmicemodels)[1]Dosage:10,20mg/kgAdministration:I.p.;dailyfor21daysResult:Significantlyanddose-dependentlysuppressedthetumorgrowthwiththeTGIratesof74.23%and94.84%atthedosageof10and20mg/kg,respectively.REFERENCES[1].RanF,etal.Developmentofnovelhydrazidoarylaminopyrimidine-basedBTK/FLT3dualinhibitorswithpotentinvivoanti-hematologicalmalignancieseffects.EurJMedChem.2023Jan5;245(Pt1):114913.McePdfHeight2/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemECaution:Producthasnotbeenfullyvalidatedformedicalapplic