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Medchemexpress/MK 2206 dihydrochloride/HY-10358/100mg

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Medchemexpress/MK 2206 dihydrochloride/HY-10358/100mg

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MedChemExpress

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HY-10358-10mM*1mLinDMSO

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4000-520-616

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MK2206isanorallyactiveallostericAktinhibitorwithIC₅₀of5nM/12nM/65nMforAkt1/Akt2/Akt3,respectively.

CustomerValidation

•Cell.2014Feb13;156(4):771-85.
•NatChemBiol.2017Jan;13(1):38-45.
•ProcNatlAcadSciUSA.2016Jul26;113(30):E4338-47.
•Oncogene.2017Aug10;36(32):4585-4596.
•BrJCancer.2017Sep26;117(7):974-983.
•HumMolGenet.2017Sep15;26(18):3553-3563.

•Oncotarget.2017Jul18;8(29):47642-47654.
•Oncotarget.2017Jan31;8(5):8536-8549.
•Oncotarget.2016May17;7(20):29131-42.
•JBiolChem.2012Mar23;287(13):9742-52.
•IntJOncol.2017Aug;51(2):625-632.
•PLoSOne.2016Jan28;11(1):e0147682.
•DevGrowthDiffer.2016Apr;58(3):280-92.
•IntJClinExpPathol.2017;10(3):3033-3042.
•Patent.US20160368910A1.
•OkayamaUniversity.2015.
•Patent.US20140309249A1.
•ChemBiol.2012Jan27;19(1):140-54.
•HarvardMedicalSchoolLINCSLIBRARY

Description

MK2206isanorallyactiveallostericAktinhibitorwithIC₅₀of5nM/12nM/65nMforAkt1/Akt2/Akt3,respectively.

IC₅₀&Target

IC50:5nM/12nM/65nM(Akt1/Akt2/Akt3)^[1]

InVitro

TheNPCcelllinesCNE-1,CNE-2,HONE-1,andSUNE-1aretreatedwithincreasingdosesofMK-2206(0-10μM)for72and96hours,resultsindose-andtime-dependentinhibitionofcellviABIlity.At72and96hours,theIC₅₀valuesofMK-2206inCNE-1,CNE-2,andHONE-1celllinesare3-5μM,andinSUNE-1,theyarelessthan1μM^[1].MK-2206alonemorepotentlyinhibitsthecellgrowthofRaswild-type(WT)celllines(A431,HCC827,andNCI-H292;IC₅₀sof5.5,4.3,and5.2μM,respectively)ascomparedwithRas-mutantcelllines(NCI-H358,NCI-H23,NCI-H1299,andCalu-6;IC₅₀sof13.5,14.1,27.0,and28.6μM,respectively),withtheexceptionofNCI-H460,whichhasaPIK3CAE545Kmutation(IC₅₀,3.4μM)^[2].

InVivo

MK-2206doses(480mg/kgonceaweekand240mg/kgthreetimesaweek)caninhibitthegrowthofhumanCNE-2xenograftsinnudemice.InthetwoMK-2206groups,thetumorweightsaremuchlighterthanthecontrolgroup(P<0.01). temporal="" body="" weight="" reduction="" is="" observed="" after="" receiving="" the="" mk-2206="">^[1].

ClinicalTrial

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References

[1].ZhaoYY,etal.EffectsofanoralallostericAKTinhibitor(MK-2206)onhumannasopharyngealcancerinvitroandinvivo.DrugDesDevelTher.2014Oct10;8:1827-37.
[2].HiraiH,etal.MK-2206,anallostericAktinhibitor,enhancesantitumorefficacybystandardchemotherapeuticagentsormoleculartargeteddrugsinvitroandinvivo.MolCancerTherapy,2010,9(7),1956-1967.
[3].JainA,etal.AblkinaseregulationbyBRAF/ERKandcooperationwithAktinmelanoma.Oncogene.2017Aug10;36(32):4585-4596.

PreparingStockSolutions

ConcentrationVolumeMass	1mg	5mg	10mg

1mM	2.0816mL	10.4082mL	20.8164mL
5mM	0.4163mL	2.0816mL	4.1633mL
10mM	0.2082mL	1.0408mL	2.0816mL

Pleaserefertothesolubilityinformationtoselecttheappropriatesolvent.

CellAssay
^[1]

MK-2206isdissolvedinDMSOandstored,andthendilutedwithappropriatemediabeforeuse^[1].

TheNPCcelllinesCNE-1,CNE-2,HONE-1,andSUNE-1areseededinto96-wellplatesatanappropriatedensityperwell.Twenty-fourhoursafterplating,varyingconcentrationsofMK-2206(0-10μM)areaddedtothewells.CellproliferationisdeterminedbyusingtheCellCountingKit8at72or96hoursafterdosing.Theopticaldensityismeasuredat450nmonanenzyme-linkedimmunosorbentassayreader.TheIC₅₀valueisdeterminedastheconcentrationresultingin50%cellgrowthinhibitionaftera72or96hoursexposuretothedrugcomparedwithuntreatedcontrolcells.Allexperimentsareperformedintriplicateinatleastthreeindependentexperiments^[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

AnimalAdmiNISTration
^[1]

30%CaptisolisusedtodosetheMK-2206^[1].

Mice^[1]
Four-tosix-week-oldmaleBALB/cnudemiceareused.CNE-2cellsat1×10⁷/mLaresUSPendedinserum-freemedium,and0.2mLmediumisinjectedsubcutaneouslyintotherightflankofeachnudemouse.Whenmeantumorvolumereachesapproximately50mm³,themicearerandomizedintothreegroups(n=7/group)withapproximatelyequivalentrangesoftumorvolumebetweengroups.TheMK-2206isdosedwith30%Captisol.MK-2206(240mg/kg,threetimesaweek),MK-2206(480mg/kg,onceaweek),and30%Captisoldiluentsareadministeredbyoralgavagefor2weeksforeachgroup.Tumorgrowthismeasuredwithcaliperseveryotherday,andthetumorvolumeiscalculatedbythefollowingformula:volume(mm³)=length×width²×0.5.Micearekilledwhenmeantumorvolumeinthecontrolgroupislargerthan2,000mm³.Harvestedtumorspecimensareweighedandfixedin10%bufferedformalinandembeddedinparaffin.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

References

[1].ZhaoYY,etal.EffectsofanoralallostericAKTinhibitor(MK-2206)onhumannasopharyngealcancerinvitroandinvivo.DrugDesDevelTher.2014Oct10;8:1827-37.
[2].HiraiH,etal.MK-2206,anallostericAktinhibitor,enhancesantitumorefficacybystandardchemotherapeuticagentsormoleculartargeteddrugsinvitroandinvivo.MolCancerTherapy,2010,9(7),1956-1967.
[3].JainA,etal.AblkinaseregulationbyBRAF/ERKandcooperationwithAktinmelanoma.Oncogene.2017Aug10;36(32):4585-4596.

MolecularWeight

480.39

Formula

C₂₅H₂₃Cl₂N₅O

CASNo.

1032350-13-2

Storage

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

Shipping

RoomtemperatureincontinentalUS;mayvaryelsewhere

Solvent&Solubility

DMSO:4.8mg/mL(Needultrasonicandwarming)

MK2206ispreparedinvehicle(30%captisol)^[3].

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

References

[1].ZhaoYY,etal.EffectsofanoralallostericAKTinhibitor(MK-2206)onhumannasopharyngealcancerinvitroandinvivo.DrugDesDevelTher.2014Oct10;8:1827-37.
[2].HiraiH,etal.MK-2206,anallostericAktinhibitor,enhancesantitumorefficacybystandardchemotherapeuticagentsormoleculartargeteddrugsinvitroandinvivo.MolCancerTherapy,2010,9(7),1956-1967.
[3].JainA,etal.AblkinaseregulationbyBRAF/ERKandcooperationwithAktinmelanoma.Oncogene.2017Aug10;36(32):4585-4596.

Purity:99.27%

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