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当前位置： 首页 > 产品中心 > Small_molecule > Medchemexpress/Navitoclax（同义词：ABT-263）/HY-10087/10mg
商品详细Medchemexpress/Navitoclax（同义词：ABT-263）/HY-10087/10mg
Medchemexpress/Navitoclax（同义词：ABT-263）/HY-10087/10mg
Medchemexpress/Navitoclax（同义词：ABT-263）/HY-10087/10mg
商品编号： HY-10087-10mM*1mLinDMSO
品牌： MedChemExp
市场价： ¥1500.00
美元价： 900.00
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
电子邮箱： info@ebiomall.com
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商品介绍
NavitoclaxisapotentandorallybioavailableBcl-2familyproteininhibitorthatbindswithhighaffinity(Ki< 1 nM) to multiple anti-apoptotic Bcl-2 family proteins including Bcl-xL,Bcl-2andBcl-w.

CustomerValidation

  • •ACSMedChemLett.2015Jun22;6(8):948-52.
Description

NavitoclaxisapotentandorallybioavailableBcl-2familyproteininhibitorthatbindswithhighaffinity(Ki<1=""nm)=""to=""multiple=""anti-apoptotic=""bcl-2=""family=""proteins=""including="">L,Bcl-2andBcl-w.

IC50&Target

Ki:<1=""nm="">L),<1=""nm=""(bcl-2),=""><1=""nm="">

InVitro

Navitoclax(ABT-263)isactiveagainstapproximatelyone-halfofthecelllinesofthePPTPinvitropanel.ThemedianIC50 forallofthelinesinthepanelis1.91µM[1].Navitoclaxincombinationwithchemotherapyagentsleadsmostovariancancercelllinesasynergisticresponse,andenhancesthecaspaseactivationatallpaclitaxeldosestestedinbothSK-OV-3andIGROV-1celllines[2].

InVivo

Navitoclax(100mg/kg/day,p.o.)alsoimprovesresponsestobendamustine-rituximab(BR)inasubsetoftumoursinmicexenograft[3].

ClinicalTrial
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References

  • [1].LockR1,etal.Initialtesting(stage1)oftheBH3mimeticABT-263bythepediatricpreclinicaltestingprogram.PediatrBloodCancer.2008Jun;50(6):1181-1189.

    [2].WongM,etal.Navitoclax(ABT-263)reducesBcl-x(L)-mediatedchemoresistanceinovariancancermodels.MolCancerTher.2012Apr;11(4):1026-1035.

    [3].AcklerS,etal.Navitoclax(ABT263)andBendamustine±RituximabInduceEnhancedKillingofNon-Hodgkin"sLymphomaTumorsinVivo.BrJPharmacol.2012Oct;167(4):881-891.

PreparingStockSolutions
ConcentrationVolumeMass1mg5mg10mg
1mM1.0261mL5.1303mL10.2605mL
5mM0.2052mL1.0261mL2.0521mL
10mM0.1026mL0.5130mL1.0261mL
Pleaserefertothesolubilityinformationtoselecttheappropriatesolvent.
KinaseAssay
[2]

Tomeasurecaspase-3/7activation,IGROV-1andSKOV3cellsareseededin96-wellplatesat5,000cellsperwell.After24hours,cellsaretreatedwithnavitoclax(1μM),paclitaxel(doserange=1-100nM),orincombinationwithnavitoclaxandpaclitaxelusingthesamedosingconcentrations.Eachtreatmentisdoneinduplicatewells.Inductionofapoptosis,followingtreatmentattime0,4,24,and48hours,isdeterminedusingaCaspase-Glo3/7assay.ADMSOcontrolisincludedinallstudies.Theexperimentisconductedtwice,andthedataarepresentedasanaverageofbothruns.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

CellAssay
[2]

NavitoclaxisdissolvedinDMSO.

Cellsareseededin384-wellplatesat3,000cellsperwell.After24hours,cellsaretreatedwithnavitoclax(doserangeof14nM-3.3μM)andpaclitaxel(doserangeof15pM-100nM)orgemcitABIne(doserangeof0.5nM-3.3μM)ina9by7matrix.Eachtreatmentiscarriedoutinquadruplicate.Cellsaretreatedfor72hours,andcellviabilityisdeterminedusingtheCellTiter-Gloassay.CellviabilityforeachtreatmentisnormalizedagainsttheDMSOcontrolgroup. MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

AnimalAdmiNISTration
[3]

NavitoclaxisadministeredbyoralgavageoncedailyinamixtureofPhosal50PG:PEG400:ethanol.

ForsystemicGranta519tumourmodels,2×106cellsareinjectedviathetailveinin0.1mLvolumeofcellmediumonday0,andtreatmentisinitiatedonday14.Allanimalsareear-taggedandmonitoredindividuallythroughouttheexperiment.NavitoclaxisadministeredbyoralgavageoncedailyinamixtureofPhosal50PG:PEG400:ethanol.Bendamustineandrituximabareadministeredi.v.at25and10mg/kg,respectively,onday1.Navitoclaxisadministeredapproximately2hbeforebendamustineandrituximab.Alltrialsarecomprisedof10micepergroup.Micearehumanelykilledwhentumoursreachedasize>2000mm3 orwhenanysignsofdistressaremonitored.Signsofdistressincludelossofambulation,labouredbreathingorweightloss>20%meanbodyweightpercage.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

References

  • [1].LockR1,etal.Initialtesting(stage1)oftheBH3mimeticABT-263bythepediatricpreclinicaltestingprogram.PediatrBloodCancer.2008Jun;50(6):1181-1189.

    [2].WongM,etal.Navitoclax(ABT-263)reducesBcl-x(L)-mediatedchemoresistanceinovariancancermodels.MolCancerTher.2012Apr;11(4):1026-1035.

    [3].AcklerS,etal.Navitoclax(ABT263)andBendamustine±RituximabInduceEnhancedKillingofNon-Hodgkin"sLymphomaTumorsinVivo.BrJPharmacol.2012Oct;167(4):881-891.

MolecularWeight

974.61

Formula

C₄₇H₅₅ClF₃N₅O₆S₃

CASNo.

923564-51-6

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

RoomtemperatureincontinentalUS;mayvaryelsewhere

Solvent&Solubility

10mMinDMSO

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

Purity:99.34%