Hotline:400-820-3792Inhibitors ? ScreeningLibraries ? Proteinswww.MedChemENVP-TNKS656(GMP)Cat.No.:HY-13990GCASNo.:1419949-20-4Synonyms:TNKS656(GMP)分子式:C??H??N?O?分子量:494.58作用靶點(diǎn):PPAR;Apoptosis作用通路:CellCycle/DNADamage;MetabolicEnzyme/Protease;VitaminDRelated/NuclearReceptor;Apoptosis儲(chǔ)存方式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY生物活性NVP-TNKS656(GMP)是GMP級(jí)別的NVP-TNKS656(HY-13990)。GMP級(jí)別的小分子可用做細(xì)胞療法中的輔助試劑。NVP-TNKS656是一種有效的，可口服的，選擇性的TNKS2抑制劑，IC50值為6nM，是PARP1和PARP2的選擇性的300多倍。體內(nèi)研究NVP-TNKS656(30or100mg/kg,p.o.)(GMP)exhibitsgoodexposureandmoderateoralbioavailabilityof32%and53%,respectively.Someslightoverproportionalincreaseinoralexposureisobservedbetween30and100mg/kgwiththedosenormalizedAUCforthe100mg/kgdosebeing2-foldhigherthanforthe30mg/kgdose.MicetreatedwithNVP-TNKS656(350mg/kg,p.o.)showgoodplasmaandtumorexposurescorrespondingtoAUC0-24hof515and325μM·h,respectively[1].REFERENCESShultzMD,etal.IdentificationofNVP-TNKS656:theuseofstructure-efficiencyrelationshipstogenerateahighlypotent,selective,andorallyactivetankyraseinhibitor.JMedChem.2013Aug22;56(16):6495-511.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel:400-820-3792Fax:021-5