BiologicalActivity
Potentandselectiveinhibitorofp38α(Kivaluesare0.5,3.6,2600and4100nMforp38α,p38β,p38γandp38δrespectively).Displays>1000-foldselectivityagainst36otherkinases;inhibitswholebloodLPS-stimulatedTNFα(IC50=3nM).Efficaciousinacuteandchronicmodelsofarthritis.
CompoundLibraries
AMG548isalsoofferedaspartoftheTocriscreenPlusandTocriscreenKinaseInhibitorToolboxI.FindoutmoreaboutcompoundlibrariesavailablefromTocris.
TechnicalData
| M.Wt | 461.56 |
| Formula | C29H27N5O |
| Storage | Storeat-20°C |
| Purity | ≥98%(HPLC) |
| CASNumber | 864249-60-5 |
| PubChemID | 11167112 |
| InChIKey | RQVKVJIRFKVPBF-VWLOTQADSA-N |
| Smiles | O=C1N(C)C(NC[C@@H](N)CC5=CC=CC=C5)=NC(C4=CC=NC=C4)=C1C3=CC2=C(C=C3)C=CC=C2 |
Thetechnicaldataprovidedaboveisforguidanceonly.ForbatchspecificdatarefertotheCertificateofAnalysis.
AllTocrisproductsareintendedforlaboratoryresearchuseonly.
SolubilityData
| Solvent | MaxConc.mg/mL | MaxConc.mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 49.8 | 100 | |
| ethanol | 49.8 | 100 |
PreparingStockSolutions
Thefollowingdataisbasedontheproductmolecularweight461.56.Batchspecificmolecularweightsmayvaryfrombatchtobatchduetosolventofhydration,whichwillaffectthesolventvolumesrequiredtopreparestocksolutions.
| Concentration/SolventVolume/Mass | 1mg | 5mg | 10mg |
|---|---|---|---|
| 1mM | 2.17mL | 10.83mL | 21.67mL |
| 5mM | 0.43mL | 2.17mL | 4.33mL |
| 10mM | 0.22mL | 1.08mL | 2.17mL |
| 50mM | 0.04mL | 0.22mL | 0.43mL |
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