BiologicalActivity
Potent,irreversIBLehumanepithelialgrowthfactorreceptor2(ErbB2)inhibitor(IC50=6nM)thatdisplays>4000-foldselectivityoverEGFR,FGFR,PDGFR,JAK1andSrc.ExhibitspotentantiproliferativeeffectsinErbB2-overexpressingcancercelllines(IC50=5nMinBT474breastcancercells)andsignificantlyinhibitsbladder,breastandprostatecancerxenograftgrowthinvivo.
CompoundLibraries
TAK165isalsoofferedaspartoftheTocriscreenPlusandTocriscreenKinaseInhibitorToolboxI.FindoutmoreaboutcompoundlibrariesavailablefromTocris.
TechnicalData
| M.Wt | 468.47 |
| Formula | C25H23F3N4O2 |
| Storage | Storeat+4°C |
| Purity | ≥99%(HPLC) |
| CASNumber | 366017-09-6 |
| PubChemID | 6444692 |
| InChIKey | ZTFBIUXIQYRUNT-MDWZMJQESA-N |
| Smiles | FC(C(C=C2)=CC=C2/C=C/C1=NC(COC3=CC=C(CCCCN4C=CN=N4)C=C3)=CO1)(F)F |
Thetechnicaldataprovidedaboveisforguidanceonly.ForbatchspecificdatarefertotheCertificateofAnalysis.
AllTocrisproductsareintendedforlaboratoryresearchuseonly.
SolubilityData
| Solvent | MaxConc.mg/mL | MaxConc.mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 35.14 | 75 |
PreparingStockSolutions
Thefollowingdataisbasedontheproductmolecularweight468.47.Batchspecificmolecularweightsmayvaryfrombatchtobatchduetosolventofhydration,whichwillaffectthesolventvolumesrequiredtopreparestocksolutions.
| Concentration/SolventVolume/Mass | 1mg | 5mg | 10mg |
|---|---|---|---|
| 1mM | 2.13mL | 10.67mL | 21.35mL |
| 5mM | 0.43mL | 2.13mL | 4.27mL |
| 10mM | 0.21mL | 1.07mL | 2.13mL |
| 50mM | 0.04mL | 0.21mL | 0.43mL |
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