BiologicalActivity
PotentEGFRandVEGFRinhibitor(IC50valuesare2,6,59,77,160and330nMforEGFR,ErbB2,VEGFR-1,VEGFR-2,ErbB4andVEGFR-3respectively).Alsoinhibitsc-Abl,c-Fmsandc-Src(IC50valuesare52,60and61nMrespectively).InhibitsproliferationofEGFRandErbB2overexpressingcancercelllinesinvitro.InhibitstumorxenograftgrowthandVEGF-inducedangiogenesisinmice.Orallyactive.
CompoundLibraries
AEE788isalsoofferedaspartoftheTocriscreenPlusandTocriscreenKinaseInhibitorToolboxII.FindoutmoreaboutcompoundlibrariesavailablefromTocris.
TechnicalData
| M.Wt | 440.58 |
| Formula | C27H32N6 |
| Storage | Storeat-20°C |
| Purity | ≥98%(HPLC) |
| CASNumber | 497839-62-0 |
| PubChemID | 10297043 |
| InChIKey | OONFNUWBHFSNBT-HXUWFJFHSA-N |
| Smiles | C[C@@H](NC2=C(C=C(C4=CC=C(CN5CCN(CC)CC5)C=C4)N3)C3=NC=N2)C1=CC=CC=C1 |
Thetechnicaldataprovidedaboveisforguidanceonly.ForbatchspecificdatarefertotheCertificateofAnalysis.
AllTocrisproductsareintendedforlaboratoryresearchuseonly.
SolubilityData
| Solvent | MaxConc.mg/mL | MaxConc.mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 44.06 | 100 |
PreparingStockSolutions
Thefollowingdataisbasedontheproductmolecularweight440.58.Batchspecificmolecularweightsmayvaryfrombatchtobatchduetosolventofhydration,whichwillaffectthesolventvolumesrequiredtopreparestocksolutions.
| Concentration/SolventVolume/Mass | 1mg | 5mg | 10mg |
|---|---|---|---|
| 1mM | 2.27mL | 11.35mL | 22.7mL |
| 5mM | 0.45mL | 2.27mL | 4.54mL |
| 10mM | 0.23mL | 1.13mL | 2.27mL |
| 50mM | 0.05mL | 0.23mL | 0.45mL |
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