PF-03758309isanATP-competitiveinhibitorofp21-activatedkinase4(PAK4),akinasetypicallyupregulatedinmanycancers.Thiscompoundexhibitsanticancerchemotherapeuticandanti-metastaticactivities.InhibitionofPAK4inhibitscellmotility,proliferation,andsurvivalincellularmodelsofcancerandsuppressestumorgrowthinanimalmodelsofcancer.PF-03758309alsoinhibitsfusionandmigrationofpreosteoclasts,osteoclastdifferentiation,andpodosomeformationincellularmodelsofosteoclast-relateddisorders.
| CasNo. | 1279034-84-2 |
|---|---|
| Purity | ≥99%,≥99%ee |
| Formula | C25H30N8OS•2HCl |
| FormulaWt. | 563.55 |
| Synonym | PF-3758309 |
| Solubility | SolubleinDMSO,waterandalcohols. |
| Appearance | Offwhitetopaleyellowpowder |
| StoreTemp | -20°C |
|---|---|
| ShipTemp | Ambient |
| InfoSheet | P2000InfoSheetPDF |
|---|
ChoiSW,YeonJT,RyuBJ,etal.RepositioningPotentialofPAK4toOsteoclasticBoneResorption.JBoneMinerRes.2015Jan31.[Epubaheadofprint].PMID:25640698.
RyuBJ,LeeH,KimSH,etal.PF-3758309,p21-activatedkinase4inhibitor,suppressesmigrationandinvasionofA549humanlungcancercellsviaregulationofCREB,NF-κB,andβ-cateninsignalingsMolCellBiochem.2014Apr;389(1-2):69-77.PMID:24366569.
MurrayBW,GuoC,PirainoJ,etal.Small-moleculep21-activatedkinaseinhibitorPF-3758309isapotentinhibitorofoncogenicsignalingandtumorgrowth.ProcNatlAcadSciUSA.2010May18;107(20):9446-51.PMID:20439741.
www.clinicaltrials.gov/show/NCT00932126
