BiologicalActivity
Potentp21-activatedkinase(PAK)inhibitor(IC50valuesare14,33,39and575nMforPAK1,PAK2,PAK3andPAK4respectively).BlocksandreversestheDISC1knockdown-inducedreductionindendriticspinesizeincorticalneurons.AttenuatesdendriticspineeliminationandenhancesspinegenerationinDISC1knockdownmice.Amelioratesautism-likebehavioralsymptomsinfragileXmentalretardation1(Fmr1)knockoutmice.Brainpenetrantandorallybioavailable.
CompoundLibraries
FRAX486isalsoofferedaspartoftheTocriscreenPlusandTocriscreenKinaseInhibitorToolboxII.FindoutmoreaboutcompoundlibrariesavailablefromTocris.
TechnicalData
| M.Wt | 513.39 |
| Formula | C25H23Cl2FN6O |
| Storage | Storeat-20°C |
| Purity | ≥98%(HPLC) |
| CASNumber | 1232030-35-1 |
| PubChemID | 68060125 |
| InChIKey | DHKFOIHIUYFSOF-UHFFFAOYSA-N |
| Smiles | FC1=CC(NC3=NC(N(CC)C(C(C5=CC=C(Cl)C=C5Cl)=C4)=O)=C4C=N3)=CC=C1N2CCNCC2 |
Thetechnicaldataprovidedaboveisforguidanceonly.ForbatchspecificdatarefertotheCertificateofAnalysis.
AllTocrisproductsareintendedforlaboratoryresearchuseonly.
SolubilityData
| Solvent | MaxConc.mg/mL | MaxConc.mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 10.27 | 20 |
PreparingStockSolutions
Thefollowingdataisbasedontheproductmolecularweight513.39.Batchspecificmolecularweightsmayvaryfrombatchtobatchduetosolventofhydration,whichwillaffectthesolventvolumesrequiredtopreparestocksolutions.
| Concentration/SolventVolume/Mass | 1mg | 5mg | 10mg |
|---|---|---|---|
| 1mM | 1.95mL | 9.74mL | 19.48mL |
| 5mM | 0.39mL | 1.95mL | 3.9mL |
| 10mM | 0.19mL | 0.97mL | 1.95mL |
| 50mM | 0.04mL | 0.19mL | 0.39mL |
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ProductDatasheets
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