BiologicalActivity
Potentpan-Trkinhibitor.DisplaysantiproliferativeeffectsincellularBa/F3assays(IC50valuesare7,9and11nMforcellscontainingthefusionproteinsTel-TrkC,Tel-TrkBandTel-TrkA,respectively).ExhibitsselectivityforTrkreceptorsoverarangeofkinases,withsomeactivityatPDGFRandc-Kit(IC50valuesare0.87and0.91μMrespectively).Orallybioavailable.
CompoundLibraries
GNF5837isalsoofferedaspartoftheTocriscreenPlus.FindoutmoreaboutcompoundlibrariesavailablefromTocris.
TechnicalData
| M.Wt | 535.49 |
| Formula | C28H21F4N5O2 |
| Storage | Storeat+4°C |
| Purity | ≥98%(HPLC) |
| CASNumber | 1033769-28-6 |
| PubChemID | 59397065 |
| InChIKey | YYDUWLSETXNJJT-MTJSOVHGSA-N |
| Smiles | O=C2NC1=CC(NC4=C(C)C=CC(NC(NC5=C(F)C=CC(C(F)(F)F)=C5)=O)=C4)=CC=C1/C2=C/C3=CC=CN3 |
Thetechnicaldataprovidedaboveisforguidanceonly.ForbatchspecificdatarefertotheCertificateofAnalysis.
AllTocrisproductsareintendedforlaboratoryresearchuseonly.
SolubilityData
| Solvent | MaxConc.mg/mL | MaxConc.mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 53.55 | 100 | |
| ethanol | 5.35 | 10 |
PreparingStockSolutions
Thefollowingdataisbasedontheproductmolecularweight535.49.Batchspecificmolecularweightsmayvaryfrombatchtobatchduetosolventofhydration,whichwillaffectthesolventvolumesrequiredtopreparestocksolutions.
| Concentration/SolventVolume/Mass | 1mg | 5mg | 10mg |
|---|---|---|---|
| 1mM | 1.87mL | 9.34mL | 18.67mL |
| 5mM | 0.37mL | 1.87mL | 3.73mL |
| 10mM | 0.19mL | 0.93mL | 1.87mL |
| 50mM | 0.04mL | 0.19mL | 0.37mL |
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