BiologicalActivity
Potent,ATP-competitiveinhibitorofRafkinases(IC50valuesare29,34and105nMforc-Raf1,B-RafV600Eandwild-typeB-Raf,respectively).DisplaysselectivityforRafkinasesoverapanelof150otherkinases;inhibitsactivationoftyrosineproteinkinasessuchasVEGFR2,Lyn,Flt1andFms.Alsoinhibitsgrowth,andinducescellcyclearrestandapoptosisincolonandmelanomacelllineswiththeB-RafV600Emutation.
LicensingInformation
SoldwiththepermissionofAstraZenecaUKLtd.
CompoundLibraries
AZ628isalsoofferedaspartoftheTocriscreenPlusandTocriscreenKinaseInhibitorToolboxII.FindoutmoreaboutcompoundlibrariesavailablefromTocris.
TechnicalData
| M.Wt | 451.52 |
| Formula | C27H25N5O2 |
| Storage | Storeat+4°C |
| Purity | ≥98%(HPLC) |
| CASNumber | 878739-06-1 |
| PubChemID | 11676786 |
| InChIKey | ZGBGPEDJXCYQPH-UHFFFAOYSA-N |
| Smiles | CC(C)(C#N)C1=CC=CC(C(NC2=CC(NC3=CC(C(N(C)C=N4)=O)=C4C=C3)=C(C)C=C2)=O)=C1 |
Thetechnicaldataprovidedaboveisforguidanceonly.ForbatchspecificdatarefertotheCertificateofAnalysis.
AllTocrisproductsareintendedforlaboratoryresearchuseonly.
SolubilityData
| Solvent | MaxConc.mg/mL | MaxConc.mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 45.15 | 100 |
PreparingStockSolutions
Thefollowingdataisbasedontheproductmolecularweight451.52.Batchspecificmolecularweightsmayvaryfrombatchtobatchduetosolventofhydration,whichwillaffectthesolventvolumesrequiredtopreparestocksolutions.
| Concentration/SolventVolume/Mass | 1mg | 5mg | 10mg |
|---|---|---|---|
| 1mM | 2.21mL | 11.07mL | 22.15mL |
| 5mM | 0.44mL | 2.21mL | 4.43mL |
| 10mM | 0.22mL | 1.11mL | 2.21mL |
| 50mM | 0.04mL | 0.22mL | 0.44mL |
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