ProductDescription
LY-2109761isanorally-bioavailablepyrrolopyrazoleinhibitoroftheTGF-b1/2kinasesubtypesinPhaseIandIIclinicalstudiesformalignantmalignancies.WithKipotenciesof38nMand300nM,respectively,LY-2109761hasbeenstudiedinmetastaticpancreaticcancercellsandcompletelyinhibitsbasalandTGF-b1-stimulatedmigrationandinvasionofL3.6pl/GLTcells.[1]LY-2109761treatmentsuppressesSmad2phosphorylationandtheSmad-dependentdownstreampathway.[2]
LY-2109761issynergisticwithgemcitABIne,significantlyprolongingsurvivaltimesandreducingtumorvolumeandmetastaticevents.[1]Additionally,LY2109761enhancesrADIationresponseandprolongssurvivalinglioblastomas.ProlliferationassaysdisplayedareductionofNMA-23cellviabilityandinhibitedself-renewalofglioblastomacancerstem-likecells(CSLC).[3]
Technicalinformation:
| ChemicalFormula: | C26H27N5O2 | |
| CAS#: | 700874-71-1 | |
| MolecularWeight: | 441.52 | |
| Purity: | >98% | |
| Appearance: | PaleBrown | |
| ChemicalName: | 7-(2-morpholinoethoxy)-4-(2-(pyridin-2-yl)-5,6-dihydro-4H-pyrrolo[1,2-b]pyrazol-3-yl)quinoline | |
| Solubility: | Upto100mMinDMSO | |
| Synonyms: | LY-2109761,LY2109761,LY2109761 |
ShippingCondition:Theproductisshippedinaglassvialatambienttemperature.
Storagecondition:Forlongershelflife,storesolidpowderat4oCdesiccated,orstoreDMSOsolutionat-20oC.
Reference:
| 1. | Melisietal.,LY2109761,anoveltransforminggrowthfactorbetareceptortypeIandtypeIIdualinhibitor,asatherapeuticapproachtosuppressingpancreaticcancermetastasis.Mol.CancerTher.2008,7(4),829-840.PubmedID:1841379 |
| 2. | Connollyetal.,ComplexitiesofTGF-?targetedcancertherapy.Int.J.Biol.Sci.2012,8(7),964-978.PubmedID:22811618 |
| 3. | Zhangetal.,BlockadeofTGF-?signalingbytheTGF?R-IkinaseinhibitorLY2109761enhancesradiationresponseandprolongssurvivalinglioblastoma.CancerRes.2011,71,7155-7167.PubmedID:22006998 |
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