Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEBarasertibCat.No.:HY-10127CASNo.:722543-31-9Synonyms:AZD1152分?式:C??H??FN?O?P分?量:587.54作?靶點(diǎn):AuroraKinase;Apoptosis作?通路:CellCycle/DNADamage;Epigenetics;Apoptosis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:≥33mg/mL(56.17mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制備儲備液1mM1.7020mL8.5101mL17.0201mL5mM0.3404mL1.7020mL3.4040mL10mM0.1702mL0.8510mL1.7020mL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，請在6個?內(nèi)使?，-20°C儲存時，請在1個?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)1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE1.請依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.17mg/mL(3.69mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.17mg/mL(3.69mM);Clearsolution3.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.17mg/mL(3.69mM);Clearsolution4.請依序添加每種溶劑：5%DMSO>>40%PEG300>>5%Tween-80>>50%salineSolubility:≥2.5mg/mL(4.26mM);Clearsolution5.請依序添加每種溶劑：5%DMSO>>95%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(4.26mM);ClearsolutionBIOLOGICALACTIVITY?物活性Barasertib(AZD1152)Barasertib-hQPA的前體藥物，?度選擇性的AuroraB抑制劑，IC50值為0.37nM。Barasertib(AZD1152)可引起癌細(xì)胞?長阻滯和凋亡。IC50&TargetAuroraB0.37nM(IC50)體外研究Barasertib-HQPA(3μM,3hours)significantlydecreasesexpressionofthephosphorylatedformsofhistoneH3infreshlyisolatedleukemiacells[1].Barasertib-hydroxyquinazolinepyrazolanilide(HQPA)]isconvertedrapidlytotheactiveBarasertib-HQPAinplasma[2].Barasertib-HQPAisusedfortheinvitroexperiments[3].Barasertib-HQPAinducesamarkedanti-propliferativeeffectaccompaniedbytheappearanceofapolyploidpopulation,whichinmostcasesledtoapoptosis[4].體內(nèi)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?邊的抑制劑?師www.MedChemE戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?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