BGC0222-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEBGC0222Cat.No.:HY-P10783分⼦式:C₁₂₄₁H₂₂₇₆N₆₄O₅₅₂分⼦量:26927.36作⽤靶点:Peptide-DrugConjugates(PDCs);Integrin作⽤通路:Antibody-drugConjugate/ADCRelated;Cytoskeleton储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY⽣物活性BGC0222⼀种新型Irinotecan(HY-16562)原药。BGC0222作为⼀种PEG-cRGD偶联的Irinotecan(HY-16562)衍⽣物，可缓慢、稳定地释放Irinotecan(HY-16562)。BGC0222与αVβ3靶点结合，其IC50值为4.25μM，针对αVβ5的IC50为58.7μM。BGC0222可诱导⾎管新⽣。BGC0222在多种肿瘤中表现出良好的抗肿瘤活性[1]。体外研究BGC0222(72h)exhibitsbetterantiproliferationactivitythanIrinotecan(HY-16562)andNKTR-102againstHT29,MIAPaCa-2andMCF-7tumorcelllines,withIC50of1.83ꢀꢀμM,3.95ꢀꢀμMand0.68ꢀꢀμM,respectively[1].BGC0222(40μM)showsgoodangiogenesisactivity,withthelengthofbloodvesselsof1930ꢀmm(CAMangiogenesisassay)[1].体内研究BGC0222(20-60mg/kg,i.v.,every4daysoronceaweek,3times)exhibitsremarkableantiproliferationactivityintheHT-29,MIAPaCa-2,NCI-H446,U-87ꢀMGandMDA-MB-231xenograftnudemice,withlowerRTVandT/CvaluesthanthatofIrinotecan(HY-16562).BGC0222(30-90mg/kg,i.v.,onceweeklyfora28-dayperiod)improvessafetyprofilerelativetoirinotecanininSprague-Dawleyrats,withthemaximumtolerateddose(MTD)of90ꢀmg/kgandlessthan60ꢀmg/kg,respectively[1].BGC0222(20-80mg/kg,i.v.,single)slowlyandsteadilyreleaseirinotecaninSprague-Dawleyrats[1].AnimalModel:HT-29,MIAPaCa-2,NCI-H446,U-87ꢀMGandMDA-MB-231xenograftfemaleBalb/cnudemice(HT-29,4ꢀ×ꢀ106;MIAPaCa-2,5ꢀ×ꢀ106;NCI-H446,8ꢀ×ꢀ106;U-87ꢀMG,4ꢀ×ꢀ106;MDA-MB-231,3ꢀ×ꢀ106)[1]Dosage:20mg/kg(MIAPaCa-2,NCI-H446,MDA-MB-231);40mg/kg(HT-29);60mg/kg(U-1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE87ꢀMG)Administration:Intravenousinjection(i.v.),every4days(HT-29andMDA-MB-231)oronceaweek(MIAPaCa-2,NCI-H446andU-87ꢀMG),3timesResult:ExhibitedremarkableantiproliferationactivityintheHT-29,MIAPaCa-2,NCI-H446,U-ꢀ87ꢀMGandMDA-MB-231xenograftnudemice.ExhibitedthatT/CvaluesofBGC0222fordays12,15,18,22,25,29and32weredeterminedtobe100%,88.8%,57.0%,27.6%,16.9%,9.87%and9.21%,whilethatofirinotecanwerefoundtobe100%,103%,93.1%,75.1%,68.8%,60.6%,71.1%intheHT-29xenograftnudemice,respectively.ShowedthattheRTVvaluesofBGC0222weremuchlowerthanthatofirinotecanandNKTR-102whentheaveragetumorsizereachedapproximately100–300ꢀmm3(afterday12)intheHT-29xenograftnudemice.REFERENCES[1].HuangYQ,etal.Design,synthesisandpharmacologicalevaluationofanovelPEG-cRGD-conjugatedirinotecanderivativeaspotentialantitumoragent.EurJMedChem.2018Oct5,158:82-90.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedical