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ABT-263isanorally-availableBcl-2familyinhibitorwithKivaluesof<1nMforBcl-2,Bcl-xL,andBcl-w.ABT-263disruptskeyBclinteractionswithproteinssuchasBim,inducingapoptosis.DespitebeingaBad-likeBh5mimetic,ABT-263hasbeenshowntopossesscytotoxicactivityandinduceapoptosisbasedprimarilyonitsBcl-2familyinhibitoryactivity.
ABT-263asastandaloneagenthasmodestactivityinlymphomaandmyelomaxenografts,butisextremelyeffectiveinenhancingtheefficacyofclinicallyrelevanttherapiessuchasrituxumabandbortezomib.(1)
Inapanelofsmallcelllungcancer(SCLC)xenografts,includingH146,H889,andH1963models,ABT-263displaysexcellentantitumoreffects,leADIngtotumorregression.(2)
Technicalinformation:
| ChemicalFormula: | C47H55ClF3N5O6S3 | |
| CAS#: | 923654-51-6 | |
| MolecularWeight: | 974.61 | |
| Purity: | >98% | |
| Appearance: | white | |
| ChemicalName: | (R)-4-(4-((4-chloro-4,4-dimethyl-3,4,5,6-tetrahydro-[1,1-biphenyl]-2-yl)methyl)piperazin-1-yl)-N-((4-((4-morpholino-1-(phenylthio)butan-2-yl)amino)-3-((trifluoromethyl)sulfonyl)phenyl)sulfonyl)benzamide | |
| Solubility: | Upto100mMinDMSO | |
| Synonyms: | ABT-263,Navitoclax,ABT263,ABT263 |
ShippingCondition:Theproductisshippedinaglassvialatambienttemperature.
Storagecondition:Forlongershelflife,storesolidpowderat4oCdesiccated,orstoreDMSOsolutionat-20oC.
Reference:
| 1. | Tseetal.,ABT-263:APotentandOrallyBioavailableBcl-2FamilyInhibitor.CancerRes.2008,68,3421-3428.PubmedID:18451170 |
| 2. | Shoemakeretal.,ActivityoftheBcl-2FamilyInhibitorABT-263inaPanelofSmallCellLungCancerXenograftModels.Clin.CancerRes.2008,14,3268-3277.PubmedID:18519752 |