• Lestaurtinibisapotentinhibitorofseveraltyrosinekinases,suchasFLT-3andTrkA,thatareassociatedwithcancergrowthandprogression.Schmidt-Arras,D.,etal."FLT-3receptortyrosinekinaseasadrugtargetinleukemia."Curr.Pharm.Des.10:1867-1883(2004).
• LestaurtinibinhibitedtumorgrowthwhenadmiNISTeredat10mg/kgs.c.b.i.d.5daysaweekfor21-28daysinPanc-1,AsPc-1,BxPc-3,Colo357,andMiaPaCa2s.c.xenograftsinathymicnudemice.Reductionsintumorgrowthvolumewere50-70%.Miknyoczki,S.J.,etal."TheTrktyrosinekinaseinhibitorCEP-701(KT-5555)exhibitssignificantantitumorefficacyinpreclinicalxenograftmodelsofhumanpancreaticductaladenocarcinoma."Clin.CancerRes.5:2205-2212(1999).
• LestaurtinibinhibitedRETandRETphosphorylationinmedullarythyroidcarcinoma(MTC)cells.ItalsoblockedthegrowthoftheseMTCcellsincultureandtumorgrowthinMTCcellxenografts.Strock,C.J.,etal."CEP-701andCEP-751InhibitConstitutivelyActivatedRETTyrosineKinaseActivityandBlockMedullaryThyroidCarcinomaCellGrowth."CancerRes.63:5559-5563(2003).
• FLT3inhibitionbylestaurtinibisassociatedwithitsclinicalactivityinAMLpatientsharboringFLT3-activatingmutations.Smith,B.D.,etal."Single-agentCEP-701,anovelFLT-3inhibitor,showsBIOLOGicandclinicalactivityinpatientswithrelapsedorrefractoryacutemyeloidleukemia."Blood103:3669-3676(2004).
• LestaurtinibisaFLT3inhibitorthatisbothpotent(IC50of2nM)andselective(noactivityontheothermembersofthetypeIIIRTKfamilyat>500nM).Levis,M.andSmall,D."NovelFLT3tyrosinekinaseinhibitors."ExpertOpin.Investig.Drugs12:1951-1962(2003).
• InTF-1/ITDcells,lestaurtinibpotentlyinhibitedthephosphorylationofFLT3/ITD(IC50< 5 nM). Lestaurtinib inhibited the proliferation of TF-1/ITD cells (IC50 ≈ 10 nM), but showed very little effect at 10 nM on TF-1 cells. Chen, P., et al. "FLT3/ITD Mutation Signaling Includes Suppression of SHP-1." J. Biol. Chem. 280: 5361-5369 (2005).
• Soldforlaboratoryormanufacturingpurposesonly;notforhuman,medical,veterinary,food,orhouseholduse.
• ThisproductisofferedforR&Duseinaccordancewith(i)35USC271(e)+A13(1)intheU.S.;(ii)Section69.1ofJapanesePatentLawinJapan;(iii)Section11,No.2oftheGermanPatentActof1981inGermany;(iv)Section60,Paragraph5boftheU.K.PatentsActof1977intheU.K.;(v)Sections55.2(1)and55.2(6)andothercommonlawexemptionsofCanADIanpatentlaw;(vi)Section68BofthePatentsActof1953inNewZealandtogetherwiththeamendmentofsamebytheStatutesAmendmentBillof2002;(vii)suchrelatedlegislationand/orcaselawasmaybeorbecomeapplicableintheaforementionedcountries;and(viii)suchsimilarlawsandrulesasmayapplyinvariousothercountries.
• Notavailableinsomecountries;notavailabletosomeinstitutions;notavailableforsomeuses.

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