BiologicalActivity
PotentLRRK2inhibitor(IC50valuesare8.9and10.1nMforLRRK2[G2019S]mutantandwild-typeLRRK2respectively).DisplaysselectivityforLRRK2overapanelof460otherkinases.BlocksSer910andSer935phosphorylationinvitroandinperipheraltissuesinvivo.Brainpenetrant.
LicensingInformation
SoldforresearchpurposesunderagreementfromGlaxoSmithKline.
CompoundLibraries
GSK2578215AisalsoofferedaspartoftheTocriscreenPlusandTocriscreenKinaseInhibitorToolboxII.FindoutmoreaboutcompoundlibrariesavailablefromTocris.
TechnicalData
| M.Wt | 399.42 |
| Formula | C24H18FN3O2 |
| Storage | StoreatRT |
| Purity | ≥99%(HPLC) |
| CASNumber | 1285515-21-0 |
| PubChemID | 68107965 |
| InChIKey | WCIGMFCFPXZRMQ-UHFFFAOYSA-N |
| Smiles | FC1=NC=CC(C2=CC=C(OCC3=CC=CC=C3)C(C(NC4=CC=CN=C4)=O)=C2)=C1 |
Thetechnicaldataprovidedaboveisforguidanceonly.ForbatchspecificdatarefertotheCertificateofAnalysis.
AllTocrisproductsareintendedforlaboratoryresearchuseonly.
SolubilityData
| Solvent | MaxConc.mg/mL | MaxConc.mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 39.94 | 100 |
PreparingStockSolutions
Thefollowingdataisbasedontheproductmolecularweight399.42.Batchspecificmolecularweightsmayvaryfrombatchtobatchduetosolventofhydration,whichwillaffectthesolventvolumesrequiredtopreparestocksolutions.
| Concentration/SolventVolume/Mass | 1mg | 5mg | 10mg |
|---|---|---|---|
| 1mM | 2.5mL | 12.52mL | 25.04mL |
| 5mM | 0.5mL | 2.5mL | 5.01mL |
| 10mM | 0.25mL | 1.25mL | 2.5mL |
| 50mM | 0.05mL | 0.25mL | 0.5mL |

