BiologicalActivity
PotentandselectiveproteinkinaseR-likeERkinase(PERK)inhibitor(IC50=0.4nM).Exhibits>1000-foldselectivityforPERKoverHR1andPKR.Inhibitsthapsigargin-inducedPERKphosphorylationinlungcarcinomaA549cells.Attenuatessubcutaneouspancreatichumantumorxenograftgrowthinmice.Orallybioavailable.
LicensingInformation
SoldforresearchpurposesonlyunderagreementfromGlaxoSmithKline
CompoundLibraries
GSK2606414isalsoofferedaspartoftheTocriscreenPlusandTocriscreenKinaseInhibitorToolboxII.FindoutmoreaboutcompoundlibrariesavailablefromTocris.
TechnicalData
| M.Wt | 451.44 |
| Formula | C24H20F3N5O |
| Storage | Storeat-20°C |
| Purity | ≥99%(HPLC) |
| CASNumber | 1337531-36-8 |
| PubChemID | 53469448 |
| InChIKey | SIXVRXARNAVBTC-UHFFFAOYSA-N |
| Smiles | NC1=NC=NC2=C1C(C3=CC(CCN4C(CC5=CC=CC(C(F)(F)F)=C5)=O)=C4C=C3)=CN2C |
Thetechnicaldataprovidedaboveisforguidanceonly.ForbatchspecificdatarefertotheCertificateofAnalysis.
AllTocrisproductsareintendedforlaboratoryresearchuseonly.
SolubilityData
| Solvent | MaxConc.mg/mL | MaxConc.mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 45.14 | 100 |
PreparingStockSolutions
Thefollowingdataisbasedontheproductmolecularweight451.44.Batchspecificmolecularweightsmayvaryfrombatchtobatchduetosolventofhydration,whichwillaffectthesolventvolumesrequiredtopreparestocksolutions.
| Concentration/SolventVolume/Mass | 1mg | 5mg | 10mg |
|---|---|---|---|
| 1mM | 2.22mL | 11.08mL | 22.15mL |
| 5mM | 0.44mL | 2.22mL | 4.43mL |
| 10mM | 0.22mL | 1.11mL | 2.22mL |
| 50mM | 0.04mL | 0.22mL | 0.44mL |
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ProductDatasheets
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