BiologicalActivity
HighaffinityandselectiveALKandROS1inhibitor(Kivaluesare<0.02,<0.07and0.7nMforROS1,wild-typeALKandALK-L1196M,respectively).Exhibits>100-foldselectivityforROS1overapanelof204otherkinases.InhibitsproliferationofBaF3cellscontainingcrizotinib-resistantROS1mutationinvitro.Inhibitstumorgrowthinrelevantmousemodels.Orallyavailableandbrainpenetrant.
LicensingInformation
SoldforresearchpurposesunderagreementfromPfizerInc.
CompoundLibraries
PF06463922isalsoofferedaspartoftheTocriscreenPlus.FindoutmoreaboutcompoundlibrariesavailablefromTocris.
TechnicalData
M.Wt | 406.41 |
Formula | C21H19FN6O2 |
Storage | Storeat-20°C |
Purity | ≥98%(HPLC) |
CASNumber | 1454846-35-5 |
PubChemID | 71731823 |
InChIKey | IIXWYSCJSQVBQM-LLVKDONJSA-N |
Smiles | C[C@@H](O3)C4=C(C=CC(F)=C4)C(N(C)CC1=NN(C)C(C#N)=C1C2=CC3=C(N)N=C2)=O |
Thetechnicaldataprovidedaboveisforguidanceonly.ForbatchspecificdatarefertotheCertificateofAnalysis.
AllTocrisproductsareintendedforlaboratoryresearchuseonly.
SolubilityData
Solvent | MaxConc.mg/mL | MaxConc.mM | |
---|---|---|---|
Solubility | |||
DMSO | 40.64 | 100 | |
ethanol | 40.64 | 100 |
PreparingStockSolutions
Thefollowingdataisbasedontheproductmolecularweight406.41.Batchspecificmolecularweightsmayvaryfrombatchtobatchduetosolventofhydration,whichwillaffectthesolventvolumesrequiredtopreparestocksolutions.
Concentration/SolventVolume/Mass | 1mg | 5mg | 10mg |
---|---|---|---|
1mM | 2.46mL | 12.3mL | 24.61mL |
5mM | 0.49mL | 2.46mL | 4.92mL |
10mM | 0.25mL | 1.23mL | 2.46mL |
50mM | 0.05mL | 0.25mL | 0.49mL |