K-Ras-PDEδ-IN-1-DataSheet-生命科學試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEK-Ras-PDEδ-IN-1Cat.No.:HY-115555CASNo.:1841464-21-8分?式:C??H??FN?O?分?量:447.5作?靶點:Phosphodiesterase(PDE)作?通路:MetabolicEnzyme/Protease儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗DMSO:12.5mg/mL(27.93mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.2346mL11.1732mL22.3464mL5mM0.4469mL2.2346mL4.4693mL10mM0.2235mL1.1173mL2.2346mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；?旦配成溶液，請分裝保存，避免反復凍融造成的產(chǎn)品失效。儲備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲存時，請在6個?內使?，-20°C儲存時，請在1個?內使?。體內實驗請根據(jù)您的實驗動物和給藥?式選擇適當?shù)娜芙?案。以下溶解?案都請先按照InVitro?式配制澄的儲備液，再依次添加助溶劑：(為保證實驗結果的可靠性，澄的儲備液可以根據(jù)儲存條件，適當保存；體內實驗的?作液，建議您現(xiàn)?現(xiàn)配，當天使?；以下溶劑前顯?的百分?指該溶劑在您配制終溶液中的體積占?；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的?式助溶)1.請依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:1.25mg/mL(2.79mM);Suspendedsolution;Needultrasonic1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEBIOLOGICALACTIVITY?物活性K-Ras-PDEδ-IN-1?種新穎的、有效的K-Ras-PDEδ抑制劑。K-Ras-PDEδ-IN-1以低納爾Kd8nM與PDEδ的法尼結合袋競爭性結合。IC50&TargetPDE48.3nM(Kd)體外研究K-Ras-PDEδ-IN-1exhibitsanIC50valueof12.3μMinPaTu8902/Panc1CTGassay[1].體內研究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