CBPD-409-DataSheet-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors • ScreeningLibraries • Proteinswww.MedChemECBPD-409Cat.No.:HY-158113分子式: C₄₆H₅₀F₂N₁₀O₅分子量: 860.95作用靶点: HistoneAcetyltransferase;PROTACs作用通路: Epigenetics;PROTAC储存方式: PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY生物活性CBPD-409是一种口服有效的CBP/p300降解剂，DC50为0.2–0.4nM。CBPD-409在AR+前列腺癌细胞系VCaP、LNCaP和22Rv1中表现出抗增殖作用，IC50为1.2–2.0nM。CBPD-409具有抗肿瘤活性(Red:CBPinhibitorGNE049(HY-108435);Blue:CRBN/cullin4AThalidomide(HY-14658);Black:Linker)[1]。体外研究CBPD-409(0.01-10nM)suppressestheARsignalingandc-MycexpressioninprostatecancercellsVCaP,LNCaPand22Rv1[1].RT-PCR[1]CellLine:VCaP,LNCaPand22Rv1Concentration:0.01-10nMIncubationTime:6hResult:ReducedmRNAlevelsofKLK3,ARandc-Myc.体内研究CBPD-409(1mg/kg,iv;3mg/kg,po)exhibitspharmacokineticprofilesinICRmice,withalowclearanceCLof1.7mL/min/kg,ahalf-lifewithT1/2of2.8h(i.v.)and2.6h(p.o.),anoralexposureCmaxof2494ng/mLandanoralbioavailabilitywithF=50%[1].CBPD-409(0.3-1mg/kg,po,oncedailyfor5weeks)exhibitsantitumorefficacyagainstVCaPprostatecancerwithtumorgrowthinhibitionTGIof73-87%,withoutsignificanttoxicityinVCaPxenograftmicemodel[1].1/2 MasterofBioactiveMolecules—您身边的抑制剂大师www.MedChemEAnimalModel:VCaPxenograftCB17SCIDmicemodel[1]Dosage:0.3-1mg/kgAdministration:p.o.,onceadayfor5weeksResult:InhibitedtumorgrowthwithTGIof73%(0.3mg/kg)and87%(1mg/kg),withoutsignificantbodyweightloss.REFERENCESChenZ,etal.,DiscoveryofCBPD-409asaHighlyPotent,Selective,andOrallyEfficaciousCBP/p300PROTACDegraderfortheTreatmentofAdvancedProstateCancer.JMedChem.2024Mar26.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel:400-820-3792