Pamiparib-BGB-290-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEPamiparibCat.No.:HY-104044CASNo.:1446261-44-4Synonyms:BGB-290分⼦式:C₁₆H₁₅FN₄O分⼦量:298.31作⽤靶点:PARP作⽤通路:CellCycle/DNADamage;Epigenetics储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:62.5mg/mL(209.51mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM3.3522mL16.7611mL33.5222mL5mM0.6704mL3.3522mL6.7044mL10mM0.3352mL1.6761mL3.3522mL请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存⽅式和期限：-80°C,6months;-20°C,1month。-80°C储存时，请在6个⽉内使⽤，-20°C储存时，请在1个⽉内使⽤。体内实验请根据您的实验动物和给药⽅式选择适当的溶解⽅案。以下溶解⽅案都请先按照InVitro⽅式配制澄的储备液，再依次添加助溶剂：(为保证实验结果的可靠性，澄的储备液可以根据储存条件，适当保存；体内实验的⼯作液，建议您现⽤现配，当天使⽤；以下溶剂前显⽰的百分⽐指该溶剂在您配制终溶液中的体积占⽐；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的⽅式助溶)1.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%saline1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:≥2.25mg/mL(7.54mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.25mg/mL(7.54mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性Pamiparib(BGB-290)⼀种有效的，具有⼝服活性的⾼选择性PARP抑制剂，对PARP1和PARP2的IC50值分别为0.9nM和0.5nM。Pamiparib能透过⾎脑屏障，可⽤于包括实体瘤在内的多种肿瘤的研究[1][2]。IC50&TargetPARP体外研究PamiparibshowspotentDNA-trappingactivitywithanIC50of13nM.Inthecellularassays,PamiparibinhibitsintracellularPARformationwithanIC50of0.24nM.TumorcelllineswithhomologousrecombinationdefectsareprofoundlysensitivetoPamiparib.PamiparibishighlyactivebothinvitroandinvivoinBRCAmutanttumors[3].体内研究PamiparibsuppressesPARPactivityinpatient-derivedglioblastomamultiformeandsmall-cell-lungcancerxenografts,andpotentiatestheeffectsofTemozolamide.InvivoactivitiesofPamiparib,anditscombinationactivitywithchemotherapiesinpatientbiopsyderivedsmallcelllungcancer(SCLC)xenograftmodels[4].户使⽤本产品发表的科研⽂献•Nature.2019Dec;576(7786):274-280.•bioRxiv.April22,2021.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].ChangyouZhou,etal.Fusedtetraorpenta-cyclicdihydrodiazepinocarbazolonesasparpinhibitors.WO2013097225A1.[2].FriedlanderM,etal.Pamiparibincombinationwithtislelizumabinpatientswithadvancedsolidtumours:resultsfromthedose-escalationstageofamulticentre,open-label,phase1a/btrial.LancetOncol.2019Sep;20(9):1306-1315.[3].ZhiyuTang,etal.Abstract1653:BGB-290:AhighlypotentandspecificPARP1/2inhibitorpotentiatesanti-tumoractivityofchemotherapeuticsinpatientbiopsyderivedSCLCmodels.CancerResearch.August2015,Volume75,Issue15.[4].ShivK.Gupta,etal.Abstract3505:InhibitionofPARPactivitybyBGB-290potentiatesefficacyofNSC362856inpatientderivedxenograftsofglioblastomamultiforme.CancerResearch.August2015,Volume75,Issue15McePdfHeightCaution:Producthasnotbeenfullyvalidatedformed