ProductDescription
PF-562271isareversIBLe,ATP-competitiveinhibitoroffocaladhesionkinase(FAK)andPyk2withanIC50of1.5and14nM,respectively.[1]Inaninduciblecell-basedassaymeasuringphospho-FAK,itrobustlyinhibitsatanIC50of5nM.Invivo,PF-562271inhibitsFAKphosphorylationinadose-dependentfashionatanEC50of93ng/mL.
PF-562271hasbeenevaluatedasapotentialtherapyforpancreaticductaladenocarcinoma[2]andforcancerpatientswithbonemetastasesandcancer-associatedosteoporosis.[3]
PF-562271hasbeenstudiedincombinationwithgemcitABIneinpancreaticcancers,andsunitinibinhepatocellularcarcinomas.[4]Inthesunitinib/PF-562271combinationstudies,bothangiogenesisandtumorproliferationwereaddressed,posingaformidableapproachtotreatingsolidtumorsoftheliver.
Technicalinformation:
| ChemicalFormula: | C21H20F3N7O3S | |
| CAS#: | 717907-75-0 | |
| MolecularWeight: | 507.49 | |
| Purity: | >98% | |
| Appearance: | White | |
| ChemicalName: | N-methyl-N-(3-((2-(2-oxoindolin-5-ylamino)-5-(trifluoromethyl)pyrimidin-4-ylamino)methyl)pyridin-2-yl)methanesulfonamide | |
| Solubility: | Upto100mMinDMSO | |
| Synonyms: | PF-562271,PF562271,PF562271 |
ShippingCondition:Theproductisshippedinaglassvialatambienttemperature.
Storagecondition:Forlongershelflife,storesolidpowderat4oCdesiccated,orstoreDMSOsolutionat-20oC.
Reference:
| 1. | Robertsetal.,Antitumoractivityandpharmacologyofaselectivefocaladhesionkinaseinhibitor,PF-562,271.CancerRes.2008,68,1935-1944PubmedID:18339875 |
| 2. | Stokesetal,.InhibitionoffocaladhesionkinasebyPF-562,271inhibitsthegrowthandmetastasisofpancreaticcancerconcomitantwithalteringthetumormicroenvironment.Mol.CancerTher.2011,10,2135-2145.PubmedID:21903606 |
| 3. | Bagietal.,Dualfocaladhesionkinase/Pyk2inhibitorhaspositiveeffectsonbonetumors:implicationsforbonemetastases.Cancer,2008,112(10),2313-2321.PubmedID:18348298 |
| 4. | Bagietal.,SunitinibandPF-562,271(FAK/Pyk2inhibitor)effectivelyblockgrowthandrecoveryofhumanhepatocellularcarcinomainaratxenograftmodel.CancerBiol.Ther.2009,8(9),856-865.PubmedID:21903606 |
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