Medchemexpress/Rapamycin(Synonyms: Sirolimus)/HY-10219/2g_蚂蚁淘，【正品极速】生物医学科研用品轻松购|ebiomall 蚂蚁淘商城

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Medchemexpress/Rapamycin(Synonyms: Sirolimus)/HY-10219/2g

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Medchemexpress/Rapamycin(Synonyms: Sirolimus)/HY-10219/2g

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MedChemExpress

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HY-10219-50mg

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4000-520-616

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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

ConcentrationVolumeMass	1mg	5mg	10mg

1mM	1.0939mL	5.4694mL	10.9389mL
5mM	0.2188mL	1.0939mL	2.1878mL
10mM	0.1094mL	0.5469mL	1.0939mL

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°C	3years
	4°C	2years
Insolvent	-80°C	6months
	-20°C	1month

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%

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