Barasertib-AZD1152-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEBarasertibCat.No.:HY-10127CASNo.:722543-31-9Synonyms:AZD1152分⼦式:C₂₆H₃₁FN₇O₆P分⼦量:587.54作⽤靶点:AuroraKinase;Apoptosis作⽤通路:CellCycle/DNADamage;Epigenetics;Apoptosis储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:≥33mg/mL(56.17mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制备储备液1mM1.7020mL8.5101mL17.0201mL5mM0.3404mL1.7020mL3.4040mL10mM0.1702mL0.8510mL1.7020mL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)1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE1.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.17mg/mL(3.69mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.17mg/mL(3.69mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.17mg/mL(3.69mM);Clearsolution4.请依序添加每种溶剂：5%DMSO>>40%PEG300>>5%Tween-80>>50%salineSolubility:≥2.5mg/mL(4.26mM);Clearsolution5.请依序添加每种溶剂：5%DMSO>>95%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(4.26mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性Barasertib(AZD1152)Barasertib-hQPA的前体药物，⾼度选择性的AuroraB抑制剂，IC50值为0.37nM。Barasertib(AZD1152)可引起癌细胞⽣长阻滞和凋亡。IC50&TargetAuroraB0.37nM(IC50)体外研究Barasertib-HQPA(3μM,3hours)significantlydecreasesexpressionofthephosphorylatedformsofhistoneH3infreshlyisolatedleukemiacells[1].Barasertib-hydroxyquinazolinepyrazolanilide(HQPA)]isconvertedrapidlytotheactiveBarasertib-HQPAinplasma[2].Barasertib-HQPAisusedfortheinvitroexperiments[3].Barasertib-HQPAinducesamarkedanti-propliferativeeffectaccompaniedbytheappearanceofapolyploidpopulation,whichinmostcasesledtoapoptosis[4].体内研究Barasertib(AZD1152,25mg/kg)markedlysuppressesthegrowthandweightsofAZD1152-treatedtumors[1].Barasertib(AZD1152,5mg/kg)enhancestheabilityofvincristineordaunorubicintoinhibittheproliferationofhumanMOLM13leukemicxenografts[1].Barasertib(AZD1152,(10-150mg/kg/d)potentlyinhibitedthegrowthofhumancolon,lung,andhematologictumorxenografts(meantumorgrowthinhibitionrange,55%toz100%;P<0.05)inimmunodeficientmice[2].AnimalModel:Femaleimmune-deficientBALB/cnudemice(MOLM13cellsinjected)[1].Dosage:5or25mg/kg.Administration:Intraperitonealinjection4timesaweekoreveryanotherday.Result:InhibitedthegrowthofhumanMOLM13cellsgrowingasxenograftsusinganimmunodeficientmurinemodel.2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE户使⽤本产品发表的科研⽂献•Science.2017Dec1;358(6367):eaan4368.•NatCommun.2019Apr18;10(1):1812•ClinCancerRes.2019Jul15;25(14):4552-4566.•AmJCancerRes.2021Jun15;11(6):3021-3038.•LeukLymphoma.2020Dec;61(14):3451-3459.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].YangJ,etal.AZD1152,anovelandselectiveauroraBkinaseinhibitor,inducesgrowtharrest,apoptosis,andsensitizationfortubulindepolymerizingagentortopoisomeraseIIinhibitorinhumanacuteleukemiacellsinvitroandinvivo.Blood.2007Sep[2].WilkinsonRW,etal.AZD1152,aselectiveinhibitorofAuroraBkinase,inhibitshumantumorxenograftgrowthbyinducingapoptosis.ClinCancerRes.2007Jun15;13(12):3682-8.[3].EvansRP,etal.TheselectiveAuroraBkinaseinhibitorAZD1152isapotentialnewtreatmentformultiplemyeloma.BrJHaematol.2008Feb;140(3):295-302.[4].OkeA,etal.AZD1152rapidlyandnegativelyaffectsthegrowthandsurvivalofhumanacutemyeloidleukemiacellsinvitroandinvivo.CancerRes.2009May15;69(10):4150-8.McePdfHeig