BiologicalActivity
Potentandselectivepan-Trkinhibitor(IC50valuesare1,2and6nMforTrkC,BandA,respectively).SelectiveforTrkoverapanelofionchannels,receptorsandotherenzymes.Peripherallyrestricted.Exhibitsefficacyinarodentmodelofinflammatorypain.Orallybioavailable.
LicensingInformation
SoldforresearchpurposesunderagreementfromPfizerInc.
TechnicalData
| M.Wt | 479.93 |
| Formula | C23H22ClN7O3 |
| Storage | StoreatRT |
| Purity | ≥98%(HPLC) |
| CASNumber | 1402438-74-7 |
| PubChemID | 66571548 |
| InChIKey | BPIWZDNVMQQBQX-UHFFFAOYSA-N |
| Smiles | NC1=NC=C2C(N(C(C)(C)CO)C=C2C(C3=CN=CC(NC(CC4=CC=C(Cl)C=N4)=O)=C3)=O)=N1 |
Thetechnicaldataprovidedaboveisforguidanceonly.ForbatchspecificdatarefertotheCertificateofAnalysis.
AllTocrisproductsareintendedforlaboratoryresearchuseonly.
SolubilityData
| Solvent | MaxConc.mg/mL | MaxConc.mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 47.99 | 100 |
PreparingStockSolutions
Thefollowingdataisbasedontheproductmolecularweight479.93.Batchspecificmolecularweightsmayvaryfrombatchtobatchduetosolventofhydration,whichwillaffectthesolventvolumesrequiredtopreparestocksolutions.
| Concentration/SolventVolume/Mass | 1mg | 5mg | 10mg |
|---|---|---|---|
| 1mM | 2.08mL | 10.42mL | 20.84mL |
| 5mM | 0.42mL | 2.08mL | 4.17mL |
| 10mM | 0.21mL | 1.04mL | 2.08mL |
| 50mM | 0.04mL | 0.21mL | 0.42mL |
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