K-Ras-PDEδ-IN-1-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEK-Ras-PDEδ-IN-1Cat.No.:HY-115555CASNo.:1841464-21-8分⼦式:C₂₅H₂₆FN₅O₂分⼦量:447.5作⽤靶点:Phosphodiesterase(PDE)作⽤通路:MetabolicEnzyme/Protease储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:12.5mg/mL(27.93mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.2346mL11.1732mL22.3464mL5mM0.4469mL2.2346mL4.4693mL10mM0.2235mL1.1173mL2.2346mL请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存⽅式和期限：-80°C,6months;-20°C,1month。-80°C储存时，请在6个⽉内使⽤，-20°C储存时，请在1个⽉内使⽤。体内实验请根据您的实验动物和给药⽅式选择适当的溶解⽅案。以下溶解⽅案都请先按照InVitro⽅式配制澄的储备液，再依次添加助溶剂：(为保证实验结果的可靠性，澄的储备液可以根据储存条件，适当保存；体内实验的⼯作液，建议您现⽤现配，当天使⽤；以下溶剂前显⽰的百分⽐指该溶剂在您配制终溶液中的体积占⽐；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的⽅式助溶)1.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:1.25mg/mL(2.79mM);Suspendedsolution;Needultrasonic1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEBIOLOGICALACTIVITY⽣物活性K-Ras-PDEδ-IN-1⼀种新颖的、有效的K-Ras-PDEδ抑制剂。K-Ras-PDEδ-IN-1以低纳尔Kd8nM与PDEδ的法尼结合袋竞争性结合。IC50&TargetPDE48.3nM(Kd)体外研究K-Ras-PDEδ-IN-1exhibitsanIC50valueof12.3μMinPaTu8902/Panc1CTGassay[1].体内研究K-Ras-PDEδ-IN-1(oralorintraperitonealinjection;10mg/kg;singledose)isindifferentvehicles(A=5%Tween-80,50%NaCl,45%H2O;B=20%DMSO,80%PEG200;C=15%DMSO,9.5%CremophorEL/EtOH(1:1),75.5%H2O)fororalandintraperitoneal(IP)administration.whereasonlyverylowcompoundlevelsarefoundinplasmaafteroraldosage,butsignificantlyhigherplasmaconcentrationsarefoundafterIPadministrationinvehicleA,BorCat10mgkg[1].K-Ras-PDEδ-IN-1(intravenousinjection;3mgkg;singledose;24hours)showsasignificantincreaseoftheplasmaexposureaswellastheterminalhalf-life(t1/2=0.4hours)whencomparestocompound93,exhibitsat1/2,CO,AUC0-tz,AUC0.inf-obs,Clobs,andVss0-inf-obsvaluesof4.1hours,2790.9ng/ml,1646.4h.ng/ml,1662.5h.ng/ml,1.8L/h/kg,5.9l/kg[1].REFERENCES[1].SandipMurarka,etal.DevelopmentofPyridazinoneChemotypesTargetingthePDEδPrenylBindingSite.Chemistry.2017May2;23(25):6083-6093.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuse