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商品描述
- PD184352isaninhibitorofmitogenactivatedproteinkinasekinase(MEKorMAPKK).
- AntitumoractivityofPD184352isevidentinpreclinicalmodels,includingpancreas,colon,andbreastcancers,whichareassociatedwithitsinhibitionofpERK.Allen,L.F.,etal."CI-1040(PD184352),atargetedsignaltransductioninhibitorofMEK(MAPKK)."Semin.Oncol.30:105-116(2003).
- PD184352profoundlyinhibitedthegrowthof,andinducedapoptosisin,ovariantumorcellswithmutationsineitherKRASorBRAF.However,ovariancancercellscontainingwild-typesequenceswerenotsensitivetoPD184352.Pohl,G.,etal."Inactivationofthemitogen-activatedproteinkinasepathwayasapotentialtarget-basedtherapyinovarianSEROustumorswithKRASorBRAFmutations."CancerRes.65:1994-2000(2005).
- PD184352inhibitedC-RafwithanIC50of12nMandinhibitedmorethan90%ofERKphosphorylationataconcentrationof10nM.Invivo,PD184352decreasedadenomaformationandsignificantlyrestoredlungstructure.Kramer,B.W.,etal."UseofmitogeniccascadeblockersfortreatmentofC-Rafinducedlungadenomainvivo:CI-1040stronglyreducesgrowthandimproveslungstructure."BMCCancer4:24(2004).
- PD184352inhibitedtheMAPKpathwayandinducedapoptosisthroughapathwayinvolvedindephosphorylation,aggregationofFas-associateddeathdomainprotein,anddeathreceptor-independentcaspase-8activation.Meng,X.W.,etal."CentralRoleofFas-associatedDeathDomainProteininApoptosisInductionbytheMitogen-activatedProteinKinaseKinaseInhibitorCI-1040(PD184352)inAcuteLymphocyticLeukemiaCellsinVitro."J.Biol.Chem.278:47326-47339(2003).
- However,PD184352sufferedfrompoorpharmacokineticsbecauseofitslowsolubilityandrapidclearance.Barrett,S.D.,etal."ThediscoveryofthebenzhydroxamateMEKinhibitorsCI-1040andPD0325901."Bioorg.Med.Chem.Lett.18:6501-6504(2008).
- 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.
RelatedTerms:
[CI-1040]M.W.478.66
C17H14ClF2IN2O2
[212631-79-3]