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当前位置： 首页 > 产品中心 > Small_molecule > Medchemexpress/雷帕霉素（同义词：西罗莫司）/HY-10219/200mg
商品详细Medchemexpress/雷帕霉素（同义词：西罗莫司）/HY-10219/200mg
Medchemexpress/雷帕霉素（同义词：西罗莫司）/HY-10219/200mg
Medchemexpress/雷帕霉素（同义词：西罗莫司）/HY-10219/200mg
商品编号： HY-10219-50mg
品牌： MedChemExp
市场价： ¥1200.00
美元价： 720.00
产地： 美国(厂家直采)
公司：
产品分类： 小分子
公司分类： Small_molecule
联系Q Q： 3392242852
电话号码： 4000-520-616
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商品介绍
RapamycinisaspecificmTORinhibitorwithIC50of0.1nM.

CustomerValidation

  • •Nature.2016Dec1;540(7631):119-123.
  • •JClinInvest.2017Sep1;127(9):3339-3352.
  • •NatCommun.2017Jun8;8:15617.
  • •StemCellReports.2017Nov23.pii:S2213-6711(17)30483-6.
  • •BiochemPharmacol.2016Dec15;122:42-61.
  • •SciRep.2017Aug14;7(1):8119.
  • •SciRep.2015Nov2;5:16024.
  • •SciBull.2015Dec;60(24):2120-2128.
  • •RespirRes.2017Jul11;18(1):136.
  • •PLoSOne.2017Nov29;12(11):e0188748.
  • •PLoSOne.2017Jun21;12(6):e0179772.
  • •OncolLett.2017Oct;14(4):4715-4721.
  • •ExpHematolOncol.2016Jul29;5:22.
  • •AmJDigestDis.2015;2(2):95-99.
  • •IntJPhysiolPathophysiolPharmacol.2015Mar20;7(1):54-60.
  • •HarvardMedicalSchoolLINCSLIBRARY
Description

RapamycinisaspecificmTORinhibitorwithIC50of0.1nM.

IC50&Target

IC50:0.1nM(mTOR)[1]

InVitro

RapamycininhibitsendogenousmTORactivityinHEK293cellswithIC50of0.1nM,morepotentlythaniRapandAP21967withIC50of5nMand10nM,respectively[1].RapamycinexertsitsantitumoreffectonmalignantgliomacellsbyinducingautophagyandsuggestthatinmalignantgliomacellsadisruptionofthePI3K/AktsignalingpathwaycouldgreatlyenhancetheeffectivenessofmTORinhibitors.RapamycininhibitscellviABIlityinallthreecelllinesinadose-dependentmanner,buttheirsensitivitiesvaried.TheIC50levelsofT98G,U87-MG,andU373-MGcellsare2nM,1μM,and>25μM,respectively[3].

InVivo

TreatmentwithRapamycin(i.p,1.5mg/kg)almostcompletelypreventsthehypertrophicincreasesinplantarismuscleweightandfibresizeat7and14days[4].WTorLS/+micearetreateddailyRapamycin(2mg/kgbodyweighti.p.)for4weeks,followsbyanadditional4weeksofweeklyinjectionsofthesamedose.ThereissignificantreversaloftheabnormalfetalgeneexpressionprofileofheartsfromRapamycin-treatedLS/+mice[5].

ClinicalTrial
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References

  • [1].EdwardsSR,etal.Therapamycin-bindingdomainoftheproteinkinasemammaliantargetofrapamycinisadestabilizingdomain.JBiolChem,2007,282(18),13395-13401.

    [2].LalicH,etal.Rapamycinenhancesdimethylsulfoxide-mediatedgrowtharrestinhumanmyelogenousleukemiacells.LeukLymphoma.2012Nov;53(11):2253-61.

    [3].TakeuchiH,etal.Synergisticaugmentationofrapamycin-inducedautophagyinmalignantgliomacellsbyphosphatidylinositol3-kinase/proteinkinaseBinhibitors.CancerRes,2005,65(8),3336-3346.

    [4].BodineSC,etal.Akt/mTORpathwayisacrucialregulatorofskeletalmusclehypertrophyandcanpreventmuscleatrophyinvivo.NatCellBiol,2001,3(11),1014-1019.

    [5].MarinTM,etal.RapamycinreverseshypertrophiccardiomyopathyinamousemodelofLEOPARDsyndrome-associatedPTPN11mutation.JClinInvest.2011Mar;121(3):1026-43.

    [6].HinoK,etal.Activin-AenhancesmTORsignalingtopromoteaberrantchondrogenesisinfibrodysplasiaossificansprogressiva.JClinInvest.2017Sep1;127(9):3339-3352.

PreparingStockSolutions
ConcentrationVolumeMass1mg5mg10mg
1mM1.0939mL5.4694mL10.9389mL
5mM0.2188mL1.0939mL2.1878mL
10mM0.1094mL0.5469mL1.0939mL
Pleaserefertothesolubilityinformationtoselecttheappropriatesolvent.
KinaseAssay
[1]

HEK293cellsareplatedat2-2.5×105cellsperwellofa12-wellplateandserum-starvedfor24hinDMEMonly.Cellsaremock-treatedortreatedwithRapamycin(0.05-50nM),iRap(0.5-500nM),orAP21967(0.5-500nM)for15minutesat37°C.Serumisaddedtoafinalconcentrationof20%for30minutesat37°C.CellsarelysedandcelllysatesareseparatedbySDS-PAGE.ResolvedproteinsaretransferredtoaPVDFmembraneandimmunoblottedwithaphosphospecificprimaryantibodyagainstThr389ofp70S6kinase.DataareanalyzedusingImageQuantandKaleidaGraph[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

CellAssay
[2]

RapamycinisdissolvedinDMSOandstored,andthendilutedwithappropriatemediumbeforeuse[2].

HL-60,NB4,U937,KG-1,andK562cellsarepassagedroutinelyinRPMI-1640supplementedwith10%heat-inactivatedFBS,2mML-glutamine,50U/mLpenicillinand50μg/mLstreptomycinina5%CO2humidifiedatmosphereat37°C.Fortheexperiments,exponentiallygrowingcellsareharvestedbycentrifugation,andresUSPendedinfreshmediumcontaining10%FBS.Thecellsareseededataninitialcelldensityof2×105/mLinBDFalconsix-wellplatesinthepresenceofvariousconcentrationsofDMSOor1μMATRA.Rapamycin(20nM)isadded20minpriortothedifferentiationagents.Atday2,0.3mLoffreshmediumisaddedtoeachwell.Theviablecellsaredeterminedbytrypanblueexclusionandquantifiedusingahemocytometer[2].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

AnimalAdmiNISTration
[4][5]

Rapamycinisdissolvedin2%carboxymethylcellulose(Rat)[4].
Rapamycinisdissolvedinethanolataconcentrationof20mg/mL,filtersterilized,resuspendedinvehicle(0.25%PEG,0.25%Tween-80)ataconcentrationof1mg/mL(Mice)[5].

Rat[4]
FemaleSprague-Dawleyrats(250-275g),theadultfemaleSDrats(225-250g)arerandomizedtotreatmentorvehiclegroupssothatthemeanstartingbodyweightsofeachgroupareequal.DrugtreatmentbeganonthedayofsurgeryoronthefirstdayofreloADIngafterthe14-daysuspension.Rapamycinisdeliveredoncedailybyintraperitonealinjectionatadoseof1.5mg/kg,dissolvedin2%carboxymethylcellulose.CsAisdeliveredoncedailybysubcutaneousinjectionatadoseof15mg/kg,dissolvedin10%methanolandoliveoil.FK506isdeliveredoncedailyviasubcutaneousinjectionatadoseof3mg/kg,dissolvedin10%ethanol,10%cremophorandsaline.
Mice[5]
Rapamycinisdissolvedinethanolataconcentrationof20mg/mL,filtersterilized,resuspendedinvehicle(0.25%PEG,0.25%Tween-80)ataconcentrationof1mg/mL,andinjectedi.p.(2mg/kgbodyweight),eitherdailyfor4weeksordailyfor4weeksfollowedbyweeklyinjectionsforanadditional4weeks.Injectionsbeganateither8weeks(priortoonsetofhypertrophy)or12weeks(afterestablishedhypertrophyisindicated)ofage,andmiceareassessedafter4weeksoftreatmentorafter8weeksoftreatment,asdetailedintheResultsandfigurelegends.Ascontrols,WTandLS/+micearetreatedwithvehiclealone.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

References

  • [1].EdwardsSR,etal.Therapamycin-bindingdomainoftheproteinkinasemammaliantargetofrapamycinisadestabilizingdomain.JBiolChem,2007,282(18),13395-13401.

    [2].LalicH,etal.Rapamycinenhancesdimethylsulfoxide-mediatedgrowtharrestinhumanmyelogenousleukemiacells.LeukLymphoma.2012Nov;53(11):2253-61.

    [3].TakeuchiH,etal.Synergisticaugmentationofrapamycin-inducedautophagyinmalignantgliomacellsbyphosphatidylinositol3-kinase/proteinkinaseBinhibitors.CancerRes,2005,65(8),3336-3346.

    [4].BodineSC,etal.Akt/mTORpathwayisacrucialregulatorofskeletalmusclehypertrophyandcanpreventmuscleatrophyinvivo.NatCellBiol,2001,3(11),1014-1019.

    [5].MarinTM,etal.RapamycinreverseshypertrophiccardiomyopathyinamousemodelofLEOPARDsyndrome-associatedPTPN11mutation.JClinInvest.2011Mar;121(3):1026-43.

    [6].HinoK,etal.Activin-AenhancesmTORsignalingtopromoteaberrantchondrogenesisinfibrodysplasiaossificansprogressiva.JClinInvest.2017Sep1;127(9):3339-3352.

MolecularWeight

914.17

Formula

C₅₁H₇₉NO₁₃

CASNo.

53123-88-9

Storage
Powder-20°C3years
 4°C2years
Insolvent-80°C6months
 -20°C1month
Shipping

RoomtemperatureincontinentalUS;mayvaryelsewhere

Solvent&Solubility

DMSO:≥28mg/mL

Rapamycinispreparedinvehicle(16%DMSOin0.5w/v%methylcellulose400)[6].

*"<1 mg/ml"="" means="" slightly="" soluble="" or="" insoluble.="" "≥"="" means="" soluble,="" but="" saturation="">

References

  • [1].EdwardsSR,etal.Therapamycin-bindingdomainoftheproteinkinasemammaliantargetofrapamycinisadestabilizingdomain.JBiolChem,2007,282(18),13395-13401.

    [2].LalicH,etal.Rapamycinenhancesdimethylsulfoxide-mediatedgrowtharrestinhumanmyelogenousleukemiacells.LeukLymphoma.2012Nov;53(11):2253-61.

    [3].TakeuchiH,etal.Synergisticaugmentationofrapamycin-inducedautophagyinmalignantgliomacellsbyphosphatidylinositol3-kinase/proteinkinaseBinhibitors.CancerRes,2005,65(8),3336-3346.

    [4].BodineSC,etal.Akt/mTORpathwayisacrucialregulatorofskeletalmusclehypertrophyandcanpreventmuscleatrophyinvivo.NatCellBiol,2001,3(11),1014-1019.

    [5].MarinTM,etal.RapamycinreverseshypertrophiccardiomyopathyinamousemodelofLEOPARDsyndrome-associatedPTPN11mutation.JClinInvest.2011Mar;121(3):1026-43.

    [6].HinoK,etal.Activin-AenhancesmTORsignalingtopromoteaberrantchondrogenesisinfibrodysplasiaossificansprogressiva.JClinInvest.2017Sep1;127(9):3339-3352.

Purity:98.98%