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 |