BiologicalActivity
Potent,selectiveinhibitorofVEGFR-2tyrosinekinase(IC50=0.9nM).Displayssomeinhibitoryactivitytowardsc-Kit,PDGFRαandFGFR-2(IC50valuesrangefrom40to170nM)butishighlyselectiveoverotherreceptortyrosinekinases(IC50>10000nMforFGFR-2,EGFRandHGFR).InhibitsVEGF-stimulatedproliferationofhumanumbilicalveinendothelialcells(HUVEC)andinhibitstumorgrowthinvivo;antiangiogenic.
CompoundLibraries
Ki8751isalsoofferedaspartoftheTocriscreenPlusandTocriscreenKinaseInhibitorToolboxI.FindoutmoreaboutcompoundlibrariesavailablefromTocris.
TechnicalData
| M.Wt | 469.41 |
| Formula | C24H18F3N3O4 |
| Storage | Storeat+4°C |
| Purity | ≥97%(HPLC) |
| CASNumber | 228559-41-9 |
| PubChemID | 11317348 |
| InChIKey | LFKQSJNCVRGFCC-UHFFFAOYSA-N |
| Smiles | COC1=C(OC)C=C2C(OC3=CC=C(NC(=O)NC4=CC=C(F)C=C4F)C(F)=C3)=CC=NC2=C1 |
Thetechnicaldataprovidedaboveisforguidanceonly.ForbatchspecificdatarefertotheCertificateofAnalysis.
AllTocrisproductsareintendedforlaboratoryresearchuseonly.
SolubilityData
| Solvent | MaxConc.mg/mL | MaxConc.mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 46.94 | 100 |
PreparingStockSolutions
Thefollowingdataisbasedontheproductmolecularweight469.41.Batchspecificmolecularweightsmayvaryfrombatchtobatchduetosolventofhydration,whichwillaffectthesolventvolumesrequiredtopreparestocksolutions.
| Concentration/SolventVolume/Mass | 1mg | 5mg | 10mg |
|---|---|---|---|
| 1mM | 2.13mL | 10.65mL | 21.3mL |
| 5mM | 0.43mL | 2.13mL | 4.26mL |
| 10mM | 0.21mL | 1.07mL | 2.13mL |
| 50mM | 0.04mL | 0.21mL | 0.43mL |
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