RO4929097isapotentandselectivesmallmoleculeinhibitorofγ-secretase(IC50=4nM),producinginhibitoryactivityofNotchsignalingintumorcells.ItinhibitsNotchprocessingintumorcellsasmeasuredbythereductionofintracellularNotchexpressionbyWesternblot.ThisleadstoreducedexpressionoftheNotchtranscriptionaltargetgeneHes1.RO4929097doesnotblocktumorcellproliferationorinduceapoptosisbutinsteadproducesalesstransformed,flattened,slower-growingphenotype.CurrentitisinphaseIstudyinpatientswithadvancedsolidtumors.
ProductCitation
NOTE:UnderlicensingagreementwithHoffmann-LaRocheLtd,thisproductistobeusedforinvitrostudyonly.
Technicalinformation:
ChemicalFormula: | C22H20F5N3O3 | |
CAS#: | 847925-91-1 | |
MolecularWeight: | 469.40 | |
Purity: | >98% | |
Appearance: | Whitesolid | |
ChemicalName: | 2,2-dimethyl-N-((S)-6-oxo-6,7-dihydro-5H-dibenzo[b,d]azepin-7-yl)-N′-(2,2,3,3,3-pentafluoro-propyl)-malonamide | |
Solubility: | Upto50mMinDMSO |
ShippingCondition:Theproductisshippedinaglassvialatambienttemperature.
Storage:Forlongershelflife,storesolidpowderat4oCdesiccated,orstoreDMSOsolutionat-20oC.
Reference:
1. | LuistroL,HeWetal.Preclinicalprofileofapotentgamma-secretaseinhibitortargetingnotchsignalingwithinvivoefficacyandpharmacodynamicproperties.CancerRes.2009;69(19):7672-80. |
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