Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemESelpercatinib-d3Cat.No.:HY-W759629CASNo.:2433775-55-2Synonyms:LOXO-292-d3分?式:C??H??D?N?O?分?量:528.62作?靶點:Isotope-LabeledCompounds;RET作?通路:Others;ProteinTyrosineKinase/RTK儲存?式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY?物活性Selpercatinib-d3(LOXO-292-d3)氘代標記的Selpercatinib.Selpercatinib(LOXO-292)?種有效的選擇性RET激酶抑制劑，抑制RET(WT)，RET(V804M)和RET(G810R)，其IC50值分別為14.0nM，24.1nM和530.7nM。Selpercatinib具有抗腫瘤作?。體外研究Stableheavyisotopesofhydrogen,carbon,andotherelementshavebeenincorporatedintodrugmolecules,largelyastracersforquantitationduringthedrugdevelopmentprocess.Deuterationhasgainedattentionbecauseofitspotentialtoaffectthepharmacokineticandmetabolicprofilesofdrugs.REFERENCES[1].RussakEM,etal.ImpactofDeuteriumSubstitutiononthePharmacokineticsofPharmaceuticals.AnnPharmacother.2019;53(2):211-216.[2].?entürkR,et,al.QuantitativebioanalyticalassayfortheselectiveRETinhibitorsselpercatinibandpralsetinibinmouseplasmaandtissuehomogenatesusingliquidchromatography-tandemmassspectrometry.JChromatogrBAnalytTechnolBiomedLifeSci.2020Jun15;1147:122131.[3].StevenW.Andrews,etal.Substitutedpyrazolo[1,5-a]pyridinecompoundsasretkinaseinhibitors.WO2018071447A1.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel:400-820-3792ax