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Selectivecheckpointkinase1(Chk1)inhibitor(Kivaluesare0.49and47nMforChk1andChk2respectively).AbrogatescellcyclearrestatSandG2-Mcheckpoints;sensitizescellstoDNAdamage.Enhancesdocetaxel(Cat.No.4056)efficacyintumorcellsandxenografts.
SoldforresearchpurposesunderagreementfromPfizerInc.
Chemicalprobes.orgisaportalthatoffersindependentguidanceontheselectionand/orapplicationofsmallmoleculesforresearch.TheuseofPF477736isreviewedonthechemicalprobeswebsite.
PF477736isalsoofferedaspartoftheTocriscreenPlusandTocriscreenKinaseInhibitorToolboxII.FindoutmoreaboutcompoundlibrariesavailablefromTocris.
Thetechnicaldataprovidedaboveisforguidanceonly.ForbatchspecificdatarefertotheCertificateofAnalysis.
AllTocrisproductsareintendedforlaboratoryresearchuseonly.
Thefollowingdataisbasedontheproductmolecularweight419.48.Batchspecificmolecularweightsmayvaryfrombatchtobatchduetosolventofhydration,whichwillaffectthesolventvolumesrequiredtopreparestocksolutions.
Referencesarepublicationsthatsupporttheproducts'biologicalactivity.
AshwellandZabludoff(2008)DNAdamagedetectionandrepairpathways-recentadvanceswithinhibitorsofcheckpointkinasesincancertherapy.Clin.CancerRes.144032PMID:18593978
Blasinaetal(2008)BreachingtheDNAdamagecheckpointviaPF-00477736,anovelsmall-moleculeinhibitorofcheckpointkinase1.Mol.CancerTher.72394PMID:18723486
Zhangetal(2009)PF-00477736mediatescheckpointkinase1signalingpathwaysandpotentiatesdocetaxel-inducedefficacyinxenografts.Clin.CancerRes.154630PMID:19584159
Keywords:PF477736,supplier,pfizer,PF477736,checkpoint,kinases,chk1,selective,inhibitors,inhibits,dna,damage,cell,cycle,arrest,abrogates,PF0044736,PF-0044736,Checkpoint,Kinases,Checkpoint,Control,Kinases,Checkpoint,Kinases,TocrisBioscience
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