ProductDescription
CX-4945isanorally-available,ATP-competitive,pyridoquinoline-basedinhibitorofCK2awithanIC50potencyof1nMandKiof0.38nM.[1,2]Inapanelof238kinasesat500nM,only7inhibitedCK2>90%[2]TreatmentofBT474andBxPC-3cellswithCX-4945ledtorapiddephosphorylationofCK2,Akt(S129),accompaniedbyreductioninphsophorylationatT308andS473ofAkt.SincenoreductioninPTENphosphorylationatCK2"sS370/S380,itissurmisedthatCX-4945suppressesPi3K/AktsignalingbydirectlyblockingphosphorylationofAktatAktatS129byCK2,ratherthanthroughactivationofPTEN.[2]
Additionally,CX-4945inhibitshypoxia-drivenhypoxiainducIBLefactor(HIF-1a)activityandpreventsdownregulationofpVHLandp53.CX-4945alsoexertsaregulatoryeffectonthesecretionofIL-6ininflammatorybreastcancer.[3]
CX-4945mayalsobeapotentialsensitizerforresistantcellstoconventionalchemotherapeuticagentssuchasgemcitABIneandcisplatin.[4]
Technicalinformation:
ChemicalFormula: | C19H12ClN3O2 | |
CAS#: | 1009820-21-6 | |
MolecularWeight: | 349.77 | |
Purity: | >99% | |
Appearance: | Yellow | |
ChemicalName: | 5-(3-chlorophenylamino)benzo[c][2,6]naphthyridine-8-carboxylicacid | |
Solubility: | Upto100mMinDMSO | |
Synonyms: | CX-4945,CX4945,CX4945,Silmitasertib |
ShippingCondition:Theproductisshippedinaglassvialatambienttemperature.
Storagecondition:Forlongershelflife,storesolidpowderat4oCdesiccated,orstoreDMSOsolutionat-20oC.
Reference:
1. | Pierreetal.,Pre-clinicalcharacterizationofCX-4945,apotentandselectivesmallmoleculeinhibitorofCK2forthetreatmentofcancer.Mol.Cell.Biochem.,2011,356,37-43.PubmedID:21755459 |
2. | Siddiqui-Jainetal.,CX-4945,anorallybioavailableselectiveinhibitorofproteinkinaseCK2,inhibitsprosurvivalandangiogenicsignalingandexhibitsantitumorefficacy.CancerRes.2010,70,10288-10298.PubmedID:21159648 |
3. | Kimetal.,DruggabilityoftheCK2inhibitorCX-4945asananticancerdrugandbeyond..Arch.Pharm.Res.2012,35(8),1293-1296.PubmedID:22941473 |
4. | Zaninetal.,EffectsoftheCK2inhibitorsCX-4945andCX-5011ondrug-resistantcells..PLosONE,2012,7(11),e49193.PubmedID:21159648 |
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