3-Methylthienyl-carbonyl-JNJ-7706621-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemE3-Methylthienyl-carbonyl-JNJ-7706621Cat.No.:HY-141685CASNo.:443798-09-2分?式:C??H??N?O?S?分?量:378.43作?靶點(diǎn):CDK;GSK-3;VEGFR;FGFR作?通路:CellCycle/DNADamage;PI3K/Akt/mTOR;StemCell/Wnt;ProteinTyrosineKinase/RTK儲(chǔ)存?式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY?物活性3-Methylthienyl-carbonyl-JNJ-7706621?種有效和選擇性的細(xì)胞周期蛋?依賴性激酶(CDK)抑制劑，對(duì)CDK1/cyclinB和CDK2/cyclinA的IC50值分別為6.4nM和2nM。3-Methylthienyl-carbonyl-JNJ-7706621還顯?出對(duì)GSK-3(IC50=0.041μM)的有效抑制和對(duì)CDK4，VEGF-R2，andFGF-R2(IC50=0.11,0.13,0.22μM)的適度效?。3-Methylthienyl-carbonyl-JNJ-7706621可?于癌癥的研究。IC50&TargetCDK2/cyclinACDK1/cyclinBCDK4FGFR22nM(IC50)6.4nM(IC50)0.11μM(IC50)0.22μM(IC50)VEGFR2GSK30.13μM(IC50)41nM(IC50)體外研究3-Methylthienyl-carbonyl-JNJ-7706621showspotentpotencyagainstGSK-3(IC50=0.041μM)andmodestpotencyagainstCDK4,VEGF-R2,andFGF-R2(IC50=0.11,0.13,0.22μM,respectively)[1].3-Methylthienyl-carbonyl-JNJ-7706621inhibitscellproliferation,withIC50sof0.28μM,0.25μM,0.45μM,0.75μM,0.59μMand0.12μMforHeLa,HCT-116,A375,SK-OV-3,MDA-MB-231andPC-3cells,respectively[1].體內(nèi)研究3-Methylthienyl-carbonyl-JNJ-7706621(75-125mg/kg;i.p.oncedailyfor32days)inhibitstheA375humanmelanomatumorgrowthandprolongsthesurvivalinnudemice[1].3-Methylthienyl-carbonyl-JNJ-7706621exhibitsoralbioavailability(nudemouse2%,rat8%,dog63.3%),terminaleliminationhalf-lives(nudemouse1.70,rat2.20and,dog2.36h)andCmax(nudemouse0.21,rat2.5,dog4.58μM)followingoraladministration(nudemouse30,rat30,dog10mg/kg)[1].1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE3-Methylthienyl-carbonyl-JNJ-7706621exhibitsterminaleliminationhalf-lives(nudemouse0.51,rat0.64and,dog3.89h),Cmax(nudemouse6.4,rat23.2,dog2.19μM)andAUC(nudemouse3.2,rat11.4,dog2.45μM?h)followingintravenousadministration(nudemouse3,rat3and,dog1mg/kg)[1].AnimalModel:MaleathymicmicewereimplantedwithA375humanmelanomacells[1]Dosage:75,100,125mg/kgAdministration:I.p.oncedailyfor32daysResult:Reducedthetumorgrowth.Survivalwasincreasedbyabout3weekscomparedwithvectoralone.REFERENCES[1].LinR,et,al.1-Acyl-1H-[1,2,4]triazole-3,5-diamineanaloguesasnovelandpotentanticancercyclin-dependentkinaseinhibitors:synthesisandevaluationofbiologicalactivities.JMedChem.2005Jun30;48(13):4208-11.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications