ForetinibisaninhibitorofROS1,MET,Ron,Axl,Tie-2,andVEGFR2thatexhibitsanticancerchemotherapeuticandanti-angiogenicactivities.Insubjectswithsquamouscellcarcinoma,foretinibdecreasestumorsize.Inhepatocellularcarcinomacells,foretinibincreasesexpressionofp27andBim,decreasesexpressionofcyclinB1andp-c-Myc,andinducesG2/Mphasecellcyclearrest,inhibitingcellgrowthandmigrationaswellastumorgrowthandangiogenesis.
| CasNo. | 849217-64-7 |
|---|---|
| Purity | ≥98% |
| Formula | C34H34F2N4O6 |
| FormulaWt. | 632.65 |
| IUPACName | 1-N"-[3-fluoro-4-[6-methoxy-7-(3-morpholin-4-ylpropoxy)quinolin-4-yl]oxyphenyl]-1-N-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide |
| Synonym | GSK-1363089,GSK1363089 |
| Solubility | Relativelyinsolubleinwaterandethanol.SolubleinDMSOto127mg/mL. |
| Appearance | Offwhitetopaleyellowpowder |
| StoreTemp | -20°C |
|---|---|
| ShipTemp | Ambient |
| MSDS | F5968MSDSPDF |
|---|---|
| InfoSheet | F5968InfoSheetPDF |
ShahMA,WainbergZA,CatenacciDV,etal.PhaseIIstudyevaluating2dosingschedulesoforalforetinib(GSK1363089),cMET/VEGFR2inhibitor,inpatientswithmetastaticgastriccancer.PLoSOne.2013;8(3):e54014.PMID:23516391.
SeiwertT,SarantopoulosJ,KallenderH,etal.PhaseIItrialofsingle-agentforetinib(GSK1363089)inpatientswithrecurrentormetastaticsquamouscellcarcinomaoftheheadandneck.InvestNewDrugs.2013Apr;31(2):417-24.PMID:22918720.
HuynhH,OngR,SooKC.Foretinibdemonstratesanti-tumoractivityandimprovesoverallsurvivalinpreclinicalmodelsofhepatocellularcarcinoma.Angiogenesis.2012Mar;15(1):59-70.PMID:22187171.
