Pirarubicin-THP-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEPirarubicinCat.No.:HY-13725CASNo.:72496-41-4Synonyms:THP分?式:C??H??NO??分?量:627.64作?靶點(diǎn):Topoisomerase;Autophagy;Bacterial;Antibiotic作?通路:CellCycle/DNADamage;Autophagy;Anti-infection儲存?式:4°C,protectfromlight*該產(chǎn)品在溶液狀態(tài)不穩(wěn)定，建議您現(xiàn)?現(xiàn)配，即刻使?。溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:10mg/mL(15.93mM;ultrasonicandwarmingandheatto80°C)MassSolvent1mg5mg10mgConcentration制備儲備液1mM1.5933mL7.9664mL15.9327mL5mM0.3187mL1.5933mL3.1865mL10mM0.1593mL0.7966mL1.5933mL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；該產(chǎn)品在溶液狀態(tài)不穩(wěn)定，建議您現(xiàn)?現(xiàn)配，即刻使?.BIOLOGICALACTIVITY?物活性Pirarubicin(THP)?種蒽環(huán)類抗?素，為拓?fù)洚悩?gòu)酶II(topoisomeraseII)的抑制劑，可?于各種癌癥尤其是實(shí)體瘤的研究。IC50&TargetTopoisomeraseII體外研究PirarubicinisatopoisomeraseIIinhibitor[1].PirarubicinshowsinhibitoryactivitiesagainstM5076andEhrlichcells,withIC50sof0.366and0.078μM,respectively.ThecytotoxicityofPirarubicintowardM5076cellsis1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemElowerthantowardEhrlichcells,andthisisduetothemuchlowerexpressionoftopoisomeraseIIinM5076cellsthaninEhrlichcells[2].Pirarubicin(2.5,5,10μg/mL)significantlyinducesautophagyinadosedependentmannerinbladdercancer(T24,EJ,5637,J82andUM-UC-3)cells.Furthmore,Pirarubicin(5μg/mL)inducesapoptosisthroughinhibitionofmTOR/p70S6K/4E-BP1inbladdercancercells,andthiseffectisenhancedbyinhibitionofautophagy[3].體內(nèi)研究Pirarubicin(18mg/kg,i.v.)significantlyelevatesserumlevelofBNP,CK-MB,CTnT,LDH,andMDAcomparedwiththoseinthecontrolgroupinacutecardiactoxicityrats.Pirarubicinalsolowersheartrate,anddepressesR-wavevoltage,andprolongationofQTintervalsintheacutecardiactoxicitymodel[4].PROTOCOLCellAssay[3]MTSisusedtoanalyzecellsurvival.Briefly,cellsareplatedin96-wellplatesintriplicateat2×103cellsperwellandculturedingrowthmedium.Thencellsaretreatedwithpirarubicinatdifferentconcentrations(2.5μg/mL,5μg/mL,10μg/mL)for24h.MTSreagent(5mg/mL)isaddedandincubatedat37°Cfor4h.Theabsorbanceismonitoredat490nmusingamicroplatereader[3].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.AnimalAnacutecardiactoxicitymodelisestablishedbyasingledoseof18mg/kgpirarubicinthroughthecaudalAdministration[4]veininjection.Thirty-sixratsarerandomizedequallytosixgroups:normalcontrol,cardiacinjury(THP)model,dexrazoxane(180mg/kg),low-doserutin(25mg/kg),middle-doserutin(50mg/kg),andhigh-doserutin(100mg/kg).Ratsintherutin-treatedgroupareadministereddifferentdosesofrutinandCMC-Nafor7daysbygavageandasingledoseof18mg/kgpirarubicinthroughcaudalveininjection.Ratsinthedexrazoxane-treatedgroupreceivesodiumcarboxymethylcellulose(CMC-Na)bygavageforsixdays.40mg/kgdexrazoxaneisthenadministeredtoratsbyintraperitonealinjectionand18mg/kgpirarubicinisadministeredbycaudalveininjectiononday7.RatsintheTHPmodelgroupreceiveCMC-Nabygavageforsevendays,followedbypirarubicin18mg/kgthroughthecaudalveininjectiononday7.RatsinthenormalcontrolgroupreceiveCMC-Nabygavageforsevendays,followedbysalinethroughcaudalveininjectiononday7[4].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?JMolLiq.2020,114633.?IntJPharm.2022May25;620:121761.?JMolMed(Berl).2019Aug;97(8):1183-1193.?Genomics.2021Nov26;S0888-7543(21)00410-9.?Heliyon.June2022,e09643.Seemorecustomervalidationsonwww.MedChemEREFERENCES2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE[1].TakigawaN,etal.CytotoxiceffectoftopoisomeraseIIinhibitorsagainstadriamycin-andetoposide-resistantsmallcelllungcancersublines.GanToKagakuRyoho.1993May;20(7):929-35.[2].NagaiK,etal.RelationshipsbetweentheinvitrocytotoxicityandtransportcharacteristicsofpirarubicinanddoxorubicininM5076ovariansarcomacells,andcomparisonwiththoseinEhrlichascitescarcinomacells.CancerChemotherPharmacol.2002Mar;49(3):244-50.Epub2002Jan8.[3].LiK,etal.Pirarubicininducesanautophagiccytoprotectiveresponsethroughsuppressionofthemammaliantargetofrapamycinsignalingpathwayinhumanbladdercancercells.BiochemBiophysResCommun.2015May1;460(2):380-5.[4].WangYD,etal.Cardioprotectiveeffectsofrutininratsexposedtopirarubicintoxicity.JAsianNatProd