ProductDescription
LBH589,ahydroxamateanalog,isabroad-spectrumHDACinhibitor.Ithasbeenshowntoincreaseacetylationofcorehistones(H3andH4)andnonhistoneproteins(alpha-tublin,HSP90),leADIngtothemodulationofgeneexpression(p21,FOXO3A,GADD45A,aromatase,etc)andproteinactivityinvolvedincellgrowthandsurvivalpathways1-4.LBH589inducesapoptosisinMOLT-4andRehcellswithIC50between5to20nM1.Inlungcancerandmesotheliomaanimalmodels,LBH589markedlydecreasedtumorgrowthby62%whencomparedwiththevehiclecontrol5.Theanti-tumoractivityofLBH589hasalsobeendemonstratedinmanyothercancercelllines,includingmultiplemyeloma,NSCLCandcastrate-resistantprostatecancercelllines.LBH589isunderclinicaltrialstoevaluateitseffectsinconjunctionwithchemotherapyand/ortargetedtherapyinmultiplecancertypes.
Technicalinformation:
| ChemicalFormula: | C21H23N3O2 | |
| CAS#: | 404950-80-7 | |
| MolecularWeight: | 349.43 | |
| Purity: | >98% | |
| Appearance: | Whitesolid | |
| ChemicalName: | (2E)-N-hydroxy-3-[4-({[2-(2-methyl-1H-indol-3-yl)ethyl]amino}methyl)phenyl]acrylamide | |
| Solubility: | Upto50mMinDMSO |
ShippingCondition:Theproductisshippedinaglassvialatambienttemperature.
Storage:Forlongershelflife,storesolidpowderat4oCdesiccated,orstoreDMSOsolutionat-20oC.
Reference:
| 1. | Scuto,A.,etal.Thenovelhistonedeacetylaseinhibitor,LBH589,inducesexpressionofDNAdamageresponsegenesandapoptosisinPh-acutelymphoblasticleukemiacells.Blood.2008May15;111(10):5093-100. |
| 2. | Chen,S.etal.TheHDACinhibitorLBH589(panobinostat)isaninhibitorymodulatorofaromatasegeneexpression.ProcNatlAcadSciUSA2010Jun15;107(24):11032-7. |
| 3. | George,P.,etal."CombinationofthehistonedeacetylaseinhibitorLBH589andthehsp90inhibitor17-AAGishighlyactiveagainsthumanCML-BCcellsandAMLcellswithactivatingmutationofFLT-3."Blood105:1768-1776(2005). |
| 4. | Qian,D.Z.,etal."Targetingtumorangiogenesiswithhistonedeacetylaseinhibitors:thehydroxamicacidderivativeLBH589."Clin.CancerRes.12:634-642(2006). |
| 5. | Crisanti,MC.etal.TheHDACinhibitorpanobinostat(LBH589)inhibitsmesotheliomaandlungcancercellsinvitroandinvivowithparticularefficacyforsmallcelllungcancer.MolCancerTher.2009Aug;8(8):2221-31. |
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