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Bpsbioscience/BMN 673/27609-2/50 mg
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产品说明
MW:380.4DaCASRegistry#:1207456-01-6Formula:C19H14F2N6OTarget:PARP1Background:BMN673hasshownanti-tumoractivitybothinvitroandinvivo.Itinhibitedproliferationoftumorcellsandxenograftswithdefectsinhomologousrecombination.ThecombinationofBMN673andDNA-damagingagentsdemonstratedsynergisticanti-tumoreffects.Inaddition,studyshowedthattheexpressionlevelsofDNArepairproteinsandstatusofPI3KpathwaypredictresponsetoBMN673insmallcelllungcancer.BMN673iscurrentlyunderinvestigationinmultipleclinicaltrialsforadvancedsolidtumorsorhematologicalmalignancies,eitherasmonotherapyorincombinationwithotheranti-tumoragents.Description:BMN673isapotentandselectivePARP1/2inhibitorwithKiof1.2and0.9nM,respectively.Synonym(s):(8R,9S)-5-fluoro-8-(4-fluorophenyl)-9-(1-methyl-1H-1,2,4-triazol-5-yl)-8,9-dihydro-1H-pyrido[4,3,2-de]phthalazin-3(2H)-onePurity:≥98%byHPLCBIOLOGicalActivity:BMN673showedIC50valueof0.57nMinenzymaticassayofPARP11.Ininvitroassay,itexhibitedgreaterpotencythanotherexistingPARPinhibitors,suchasveliparib,rucaparib,andolaparib.ItismuchmorepotentattrappingPARP-DNAcomplexesthanotherPARPinhibitors.Solubility:SolubleinDMSOStorage/StABIlity:Storeatorbelow–20°C.Solidformisstableatleast12monthsfromdateofreceipt,whenstoredasdirected.Donotstoreaqueoussolutionsformorethanoneday.Reference(s):1.ShenY,etal.ClinCancerRes2013;19:5003-5015.2.CardnellRJ,etal.ClinCancerRes2014;20:2237.3.MuraiJ,etal.MolCancerTher2014;13:433-443.4.CardnellRJ,etal.ClinCancerRes2013;19:6322-6328.ScientificCategory:PARPInhibitorProductType:InhibitorDatashownislot-specific.Contactusforspecificinformationonotherlots.
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