Talazoparib-BMN-673-DataSheet-生命科學試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemETalazoparibCat.No.:HY-16106CASNo.:1207456-01-6Synonyms:BMN-673;LT-673分?式:C??H??F?N?O分?量:380.35作?靶點: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)體外實驗DMSO:25mg/mL(65.73mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.6292mL13.1458mL26.2916mL5mM0.5258mL2.6292mL5.2583mL10mM0.2629mL1.3146mL2.6292mL請根據(jù)產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，避免反復凍融造成的產品失效。儲備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲存時，請在6個?內使?，-20°C儲存時，請在1個?內使?。體內實驗請根據(jù)您的實驗動物和給藥?式選擇適當?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：(為保證實驗結果的可靠性，澄的儲備液可以根據(jù)儲存條件，適當保存；體內實驗的?作液，建議您現(xiàn)?現(xiàn)配，當天使?；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：1%DMSO>>99%saline1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:≥0.25mg/mL(0.66mM);Clearsolution2.請依序添加每種溶劑：10%DMAC>>6%SolutolHS-15>>84%PBSSolubility:5mg/mL(13.15mM);Suspendedsolution;Needultrasonic3.請依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.5mg/mL(6.57mM);Clearsolution4.請依序添加每種溶劑：2%DMSO>>40%PEG300>>5%Tween-80>>53%salineSolubility:≥0.5mg/mL(1.31mM);Clearsolution5.請依序添加每種溶劑：5%DMSO>>95%(20%SBE-β-CDinsaline)Solubility:1.25mg/mL(3.29mM);Suspendedsolution;NeedultrasonicBIOLOGICALACTIVITY?物活性Talazoparib(BMN-673)?種?效的，具有?服活性的PARP1/2抑制劑。Talazoparib抑制PARP1和PARP2酶活性的Ki值分別為1.2nM和0.87nM。Talazoparib具有抗腫瘤活性[1]。IC50&TargetPARP2PARP10.87nM(Ki)1.2nM(Ki)體外研究TalazoparibshowsanEC50of2.51nMincellularPARylationassay[1].TalazoparibshowsEC50sof0.3nM,5nMand0.31forMX-1cells(BRCA1mutant),Capan-1cells(BRCA2mutant)andMRC-5cells(normal)[1].體內研究Talazoparib(0.33mg/kg;i.g.;oncedaily;for28days)exhibitsantitumoractivityagainstBRCA1mutantbreastcancermodelinmice[1].Talazoparibexhibitsmoderateoralbioavailability(rat56%)andCmax(rat7948ng/mL)followingoraladministration(rat10mg/kg)[1].Talazoparibexhibitstheterminaleliminationhalf-life(rat2.25h)duetoplasmaclearance(2mL/min/kg)followingintravenousadministration(rat5mg/kg)[1].AnimalModel:Femaleathymicnu/numice(8-10weeksold),withMX-1xenograft-bearingmice[1]Dosage:0.33mg/kgAdministration:Oralgavage,oncedaily,for28daysResult:SignificantlyinhibitedxenograftMX-1tumorgrowth.AnimalModel:Sprague-Dawleyrats[1]Dosage:5mg/kgfori.v.;10mg/kgfororal(PharmacokineticAnalysis)Administration:IntravenousadministrationandoraladministrationResult:Oralbioavailability(56%),Cmax(7948ng/mL),T1/2(2.25h).2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE戶使?本產品發(fā)表的科研?獻?NatGenet.2022Dec5.?CancerCell.2020Dec14;38(6):844-856.e7.?CancerDiscov.2022May12;candisc.1181.2021.?CancerDiscov.2017Sep;7(9):984-998.?NatCancer.2022Oct;3(10):1211-1227.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].WangB,etal.DiscoveryandCharacterizationof(8S,9R)-5-Fluoro-8-(4-fluorophenyl)-9-(1-methyl-1H-1,2,4-triazol-5-yl)-2,7,8,9-tetrahydro-3H-pyrido[4,3,2-de]phthalazin-3-one(BMN673,Talazoparib),aNovel,HighlyPotent,andOrallyEfficaciousPoly(ADP-[2].ShenY,etal.BMN673,anovelandhighlypotentPARP1/2inhibitorforthetreatmentofhumancancerswithDNArepairdeficiency.ClinCancerRes.2013Sep15;19(18):5003-15.McePdfHeightCaution:Producthasn