CP868596(Crenolanib)isanorally-available,benzimidazole-basedinhibitorofPDGFRaandPDGFRbwithIC50valuesof0.9and1.8nM,respectively.FurThermore,CP868596isactiveagainsttheD842VmutantofPDGFRa,inhibitingphosphorylationatanIC50rangeof10-30nM(wild-typePDGFRaIC50=10nM).[1]Whereasimatinib,sunitinib,sorafenib,andnilotinibhavelittletonoactivityvs.thisD842Vmutant,CP868596offersanoveltherapytoGISTpatientswiththisresistance.

CP868596alsoshowspotency(IC50=80nM)againstthehighlysensitiveH1703cellline,suggestingsingle-agenttherapypotentialforPDGFR-drivenNSCLCtumors.[2]

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Technicalinformation:

ChemicalFormula:		C26H29N5O2
CAS#:		670220-88-9
MolecularWeight:		443.54
Purity:		>98%
Appearance:		White
ChemicalName:		1-(2-(5-((3-methyloxetan-3-yl)methoxy)-1H-benzo[d]imidazol-1-yl)quinolin-8-yl)piperidin-4-amine
Solubility:		Upto100mMinDMSO
Synonyms:		CP-868569,CP868596,CP868569,Crenolanib

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ShippingCondition:Theproductisshippedinaglassvialatambienttemperature.
Storagecondition:Forlongershelflife,storesolidpowderat4^oCdesiccated,orstoreDMSOsolutionat-20^oC.

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Reference:

1.	"Crenolanib(CP-868,596),aHighlyPotentPDGFRInhibitor,InhibitsPhosphorylationoftheImatinib-ResistantPDGFR?(D842V)ActivatingMutationAssociatedwithAdvancedGIST"AROGPharmaceuticalsandOregonHealth&ScienceUniversity,AACRposter,2011,Abstract3586.
2.	"Crenolanib(CP-868,596),ahighlypotentandselectivePDGFRTKIinhibitsgrowthofPDGFR?-drivenlungcancercells"AROGPharmaceuticalsandSouthwesternMedicalCenter,AACRposter,2011,Abstract3601.

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