BiologicalActivity
Selectiveinhibitoroffarnesyltransferase(FTase).BlocksfarnesylationofH-Ras,N-RasandK-Ras4B(IC50valuesare0.8,1.2and2.0nMrespectively).Displays>50,000-foldselectivityforFTaseovergeranylgeranyltransferase(GGTase)I.InhibitsVEGF-inducedRasactivation;suppressesangiogenesisinvivoandinvitro(IC50=75nM).Orallyactive.
CompoundLibraries
LB42708isalsoofferedaspartoftheTocriscreenPlus.FindoutmoreaboutcompoundlibrariesavailablefromTocris.
TechnicalData
| M.Wt | 555.46 |
| Formula | C30H27BrN4O2 |
| Storage | DesiccateatRT |
| Purity | ≥98%(HPLC) |
| CASNumber | 226929-39-1 |
| PubChemID | 10099206 |
| InChIKey | GUUIRIMAQGOLHT-UHFFFAOYSA-N |
| Smiles | O=C(N4CCOCC4)C1=CN(CC5=CN=CN5CC6=CC=C(Br)C=C6)C=C1C2=CC=CC3=C2C=CC=C3 |
Thetechnicaldataprovidedaboveisforguidanceonly.ForbatchspecificdatarefertotheCertificateofAnalysis.
AllTocrisproductsareintendedforlaboratoryresearchuseonly.
SolubilityData
| Solvent | MaxConc.mg/mL | MaxConc.mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 55.55 | 100 | |
| ethanol | 55.55 | 100 |
PreparingStockSolutions
Thefollowingdataisbasedontheproductmolecularweight555.46.Batchspecificmolecularweightsmayvaryfrombatchtobatchduetosolventofhydration,whichwillaffectthesolventvolumesrequiredtopreparestocksolutions.
| Concentration/SolventVolume/Mass | 1mg | 5mg | 10mg |
|---|---|---|---|
| 1mM | 1.8mL | 9mL | 18mL |
| 5mM | 0.36mL | 1.8mL | 3.6mL |
| 10mM | 0.18mL | 0.9mL | 1.8mL |
| 50mM | 0.04mL | 0.18mL | 0.36mL |
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ProductDatasheets
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