Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEBarasertib-HQPACat.No.:HY-10126CASNo.:722544-51-6Synonyms:AZD2811;INH-34;AZD1152-HQPA分?式:C??H??FN?O?分?量:507.56作?靶點(diǎn):AuroraKinase;Apoptosis作?通路:CellCycle/DNADamage;Epigenetics;Apoptosis儲(chǔ)存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:≥22mg/mL(43.34mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM1.9702mL9.8511mL19.7021mL5mM0.3940mL1.9702mL3.9404mL10mM0.1970mL0.9851mL1.9702mL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(chǔ)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(chǔ)備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲(chǔ)存時(shí)，請?jiān)?個(gè)?內(nèi)使?，-20°C儲(chǔ)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(dòng)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(chǔ)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(chǔ)備液可以根據(jù)儲(chǔ)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:≥2.5mg/mL(4.93mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(4.93mM);ClearsolutionBIOLOGICALACTIVITY?物活性Barasertib-HQPA(AZD2811)?種?度選擇性的極光激酶B抑制劑，在?細(xì)胞試驗(yàn)中IC50值為0.37nM。Barasertib-HQPA(AZD2811)對可引起癌細(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-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.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].戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?Science.2017Dec1;358(6367):eaan4368.?SciTranslMed.2018Jul18;10(450).pii:eaaq1093.2/3MasterofBioactiveMolecules—您?邊的抑制劑?師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