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苏州工业园区生物纳米园A4#216
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4000-520-616 / 18915418616
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0512-67156496
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商品描述
ProductDescription
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]
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 |
ShippingCondition:Theproductisshippedinaglassvialatambienttemperature.
Storagecondition:Forlongershelflife,storesolidpowderat4oCdesiccated,orstoreDMSOsolutionat-20oC.
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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