eCF506-d5-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors • ScreeningLibraries • Proteinswww.MedChemEeCF506-d5Cat.No.:HY-112096S分子式: C₂₆H₃₃D₅N₈O₃分子量: 515.66作用靶点: Src;Isotope-LabeledCompounds作用通路: ProteinTyrosineKinase/RTK;Others储存方式: PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY生物活性eCF506-d5是氘代标记的eCF506(HY-112096)。eCF506是高效，有口服活性的非受体酪氨酸激酶Src的抑制剂，IC50值小于0.5nM。体外研究Stableheavyisotopesofhydrogen,carbon,andotherelementshavebeenincorporatedintodrugmolecules,largelyastracersforquantitationduringthedrugdevelopmentprocess.Deuterationhasgainedattentionbecauseofitspotentialtoaffectthepharmacokineticandmetabolicprofilesofdrugs[1].eCF506inducesaverypotentantiproliferativeeffectinbothMCF7andMDA-MB-231cells.eCF506inhibitsphosphorylationofSRCandFAKatlownanomolarlevels,withcompleteinhibitionobservedat100nM.eCF506significantlyreducescellmotilityat10nMasearlyas6hintothestudy,withequivalentefficacytodasatinib.eCF506exclusivelyinhibitsSFK,withsubnanomolarIC50valuesagainstSRCandYES(IC50=0.5,2.1nM).ItisimportanttohighlightthateCF506displaysavastdifferenceinactivity(>950-folddifference)betweenABLanditsprimarytargetSRC[2].体内研究eCF506showsamoderateoralbioavailability(25.3%).Asignificantreductionofphospho-SRCY416isobservedinthexenograftsectionsfrommicetreatedwitheCF506relativetotheuntreatedanimalcontrols[2].REFERENCESFraserC,etal.RapidDiscoveryandStructure-ActivityRelationshipsofPyrazolopyrimidinesThatPotentlySuppressBreastCancerCellGrowthviaSRCKinaseInhibitionwithExceptionalSelectivityoverABLKinase.JMedChem.2016May26;59(10):4697-710.RussakEM,etal.ImpactofDeuteriumSubstitutiononthePharmacokineticsofPharmaceuticals.AnnPharmacother.2019Feb;53(2):211-216.McePdfHeight1/1 MasterofBioactiveMolecules—您身边的抑制剂大师www.MedChemECaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel:40