ProductDescription
SU-11274isanoxindole-based,ATP-competitive,Metinhibitorwithactivityof20nMandis>500-foldselectiveagainstavarietyofotherkinasessuchasPDGFR,EGFR,cdk2,src,andFGFR.[1]SU11274inducesG1cellcyclearrestandapoptosiswithincreasedcaspase3activity.ReductionofphosphorylationinthePI3KandRaspathwaycomponents,suchasAkt,GSK-3,andFKHR.[1]SU11274inhibitscellviABIlity,c-Met/HGFanddownstreamcellproliferationinc-Met-expressingNSCLCcells.[2]
Morerecently,SU11274hasbeenextensivelystudiedforthetreatmentofhepatocellularcarcinoma(HCC).Inparticular,cellspostiivefordes-gamma-carboxyprothrombin(DCP),anagentthatinteractswithc-MettoactivateHCCcellgrowth,wereinhibitedbySU11274.[3]
Technicalinformation:
| ChemicalFormula: | C28H30CIN5O4S | |
| CAS#: | 658084-23-2 | |
| MolecularWeight: | 568.09 | |
| Purity: | >98% | |
| Appearance: | Yellow | |
| ChemicalName: | (Z)-N-(3-chlorophenyl)-3-((3,5-dimethyl-4-(1-methylpiperazine-4-carbonyl)-1H-pyrrol-2-yl)methylene)-N-methyl-2-oxoindoline-5-sulfonamide | |
| Solubility: | Upto100mMinDMSO | |
| Synonyms: | SU11274,SU-11274 |
ShippingCondition:Theproductisshippedinaglassvialatambienttemperature.
Storagecondition:Forlongershelflife,storesolidpowderat4oCdesiccated,orstoreDMSOsolutionat-20oC.
Reference:
| 1. | Sattleretal.,AnovelsmallmoleculemetinhibitorinducesapoptosisincellstransformedbytheoncogenicTPR-METtyrosinekinase.CancerRes.2003,63,5462-5469.PubmedID:14500382 |
| 2. | Maetal.,Functionalexpressionandmutationsofc-MetanditstherapeuticinhibitionwithSU11274andsmallinterferingRNAinnon-smallcelllungcancer.CancerRes.2005,65,1479-1488.PubmedID:15735036 |
| 3. | Inagakietal.,Effectofc-MetinhibitorSU11274onhepatocellularcarcinomacellgrowth.BioScienceTrends2011,5(2),52-56.PubmedID:21572247 |
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