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Imatinibisanorally-available,aminopyrimidine-basedinhibitorofAbl,c-Kit,andPDGFRwithcellularphosphorylationinhibitionIC50valueof0.1uM.[1]
Focusedstudiesonc-KitshowthatImatinibinhibitsactivityofbothwild-typeandmutantc-Kit,aswellasc-Kit-dependentactivationofAkt.[2]FurThermore,ImatinibcompletelysuppressesactivationofMAPKandtheantiapoptoticeffectofc-Kitactivation.
StudiesonthePDGFreceptorsshowthatImatinibpreferentiallyinhibitsthebothaandbisoforms,butnotthecloselyrelatedc-Fms,Flt3,KDR,Flt1,andTEKtyrosinekinases.[3]Inaddition,Imatinibinhibitsstemcellfactor-mediatedcellularsignalling,includingligand-stimulatedreceptorautophosphorylationandinositolphosphateformation.
Technicalinformation:
| ChemicalFormula: | C29H31N7O.CH4SO3 | |
| CAS#: | 220127-57-1 | |
| MolecularWeight: | 589.4 | |
| Purity: | >99% | |
| Appearance: | White | |
| ChemicalName: | 4-[(4-Methyl-1-piperazinyl)methyl]-N-[4-methyl-3-[[4-(3-pyridinyl)-2-pyrimidinyl]amino]phenyl]benzamideMethanesulfonate | |
| Solubility: | Upto22mMinDMSO | |
| Synonyms: | STI-571,STI571,STI571,Imatinibmesylate,Gleevec,Glivec |
ShippingCondition:Theproductisshippedinaglassvialatambienttemperature.
Storagecondition:Forlongershelflife,storesolidpowderat4oCdesiccated,orstoreDMSOsolutionat-20oC.
Reference:
| 1. | Capdevilleetal.,Glivec(STI571,imatinib),arationallydeveloped,targetedanticancerdrug.Nat.Rev.Drug.Disc.2002,1,493-502.PubmedID:12120256 |
| 2. | Heinrichetal.,Inhibitionofc-kitreceptortyrosinekinaseactivitybySTI571,aselectivetyrosinekinaseinhibitor.Blood,2000,96(3),925-932.PubmedID:10910906 |
| 3. | Buchdungeretal.,Ablprotein-tyrosinekinaseinhibitorSTI571inhibitsinvitrosignaltransductionmediatedbyc-kitandplatelet-derivedgrowthfactorreceptors.J.Pharmacol.Exp.Ther.2000,295(1),139-145.PubmedID:10991971 |