Barasertib-HQPA-AZD2811-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEBarasertib-HQPACat.No.:HY-10126CASNo.:722544-51-6Synonyms:AZD2811;INH-34;AZD1152-HQPA分⼦式:C₂₆H₃₀FN₇O₃分⼦量:507.56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:≥22mg/mL(43.34mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制备储备液1mM1.9702mL9.8511mL19.7021mL5mM0.3940mL1.9702mL3.9404mL10mM0.1970mL0.9851mL1.9702mL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:≥2.5mg/mL(4.93mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(4.93mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性Barasertib-HQPA(AZD2811)⼀种⾼度选择性的极光激酶B抑制剂，在⾮细胞试验中IC50值为0.37nM。Barasertib-HQPA(AZD2811)对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-HQPAtreatmentinduceddefectivecellsurvival,polyploidy,andcelldeathinLNCaPcellline[3].Barasertib-HQPAinducesamarkedanti-propliferativeeffectaccompaniedbytheappearanceofapolyploidpopulation,whichinmostcasesledtoapoptosis[4].CellProliferationAssay[1].CellLine:AMLlines(HL-60,NB4,MOLM13),ALLline(PALL-2),biphenotypicleukemia(MV4-11),acuteeosinophilicleukemia(EOL-1),andtheblastcrisisofchronicmyeloidleukemiaK562cells.Concentration:0-100nM.(Barasertib-HQPA)IncubationTime:48h.Result:IC50valuesrangedfrom3nMto40nM.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].户使⽤本产品发表的科研⽂献•Science.2017Dec1;358(6367):eaan4368.•SciTranslMed.2018Jul18;10(450).pii:eaaq1093.2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE•IntJMolSci.2022,23(2),763.•JCellSci.2019Jul1;132(13):jcs229385.•ExpCellRes.2021Jul21;112741.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].WilkinsonRW,etal.AZD1152,aselectiveinhibitorofAuroraBkinase,inhibitshumantumorxenograftgrowthbyinducingapoptosis.ClinCancerRes.2007Jun15;13(12):3682-8.[2].Yang,Jing.,etal.AZD1152,anovelandselectiveauroraBkinaseinhibitor,inducesgrowtharrest,apoptosis,andsensitizationfortubulindepolymerizingagentortopoisomeraseIIinhibitorinhumanacuteleukemiacellsinvitroandinvivo.Blood.200[3].ZekriA,etal.AZD1152-HQPAinducesgrowtharrestandapoptosisinandrogen-dependentprostatecancercellline(LNCaP)viaproducinganeugenicmicronucleiandpolyploidy.TumourBiol.2015Feb;36(2):623-32.[4].OkeA,etal.AZD1152rapidlyandnegativelyaffectsthegrowthandsurvivalofhumanacutemyeloidleukemiacellsinvitroandinvivo.CancerRes.2009May15;69(10):4150-8.McePdfHeightCautio