Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEPamiparibCat.No.:HY-104044CASNo.:1446261-44-4Synonyms:BGB-290分?式:C??H??FN?O分?量:298.31作?靶點(diǎn):PARP作?通路:CellCycle/DNADamage;Epigenetics儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:62.5mg/mL(209.51mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM3.3522mL16.7611mL33.5222mL5mM0.6704mL3.3522mL6.7044mL10mM0.3352mL1.6761mL3.3522mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；?旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲存時(shí)，請?jiān)?個(gè)?內(nèi)使?，-20°C儲存時(shí)，請?jiān)?個(gè)?內(nèi)使?。體內(nèi)實(shí)驗(yàn)請根據(jù)您的實(shí)驗(yàn)動物和給藥?式選擇適當(dāng)?shù)娜芙?案。以下溶解?案都請先按照InVitro?式配制澄的儲備液，再依次添加助溶劑：(為保證實(shí)驗(yàn)結(jié)果的可靠性，澄的儲備液可以根據(jù)儲存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的?作液，建議您現(xiàn)?現(xiàn)配，當(dāng)天使?；以下溶劑前顯?的百分?指該溶劑在您配制終溶液中的體積占?；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的?式助溶)1.請依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%saline1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:≥2.25mg/mL(7.54mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.25mg/mL(7.54mM);ClearsolutionBIOLOGICALACTIVITY?物活性Pamiparib(BGB-290)?種有效的，具有?服活性的?選擇性PARP抑制劑，對PARP1和PARP2的IC50值分別為0.9nM和0.5nM。Pamiparib能透過?腦屏障，可?于包括實(shí)體瘤在內(nèi)的多種腫瘤的研究[1][2]。IC50&TargetPARP體外研究PamiparibshowspotentDNA-trappingactivitywithanIC50of13nM.Inthecellularassays,PamiparibinhibitsintracellularPARformationwithanIC50of0.24nM.TumorcelllineswithhomologousrecombinationdefectsareprofoundlysensitivetoPamiparib.PamiparibishighlyactivebothinvitroandinvivoinBRCAmutanttumors[3].體內(nèi)研究PamiparibsuppressesPARPactivityinpatient-derivedglioblastomamultiformeandsmall-cell-lungcancerxenografts,andpotentiatestheeffectsofTemozolamide.InvivoactivitiesofPamiparib,anditscombinationactivitywithchemotherapiesinpatientbiopsyderivedsmallcelllungcancer(SCLC)xenograftmodels[4].戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?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