BiologicalActivity
Potentinhibitorofc-METandanaplasticlymphomakinase(ALK)(cellIC50valuesare8.0and20nMrespectively).Selectiveforc-METandALKagainst>120differentkinases.Displaysantitumorefficacyinmultipletumormodels;inhibitsc-MET-dependentproliferation,migrationandinvasionofhumantumorcellsinvitro.Orallybioavailable.
LicensingInformation
SoldforresearchpurposesunderagreementfromPfizerInc.
TechnicalData
| M.Wt | 450.34 |
| Formula | C21H22Cl2FN5O |
| Storage | Storeat+4°C |
| Purity | ≥99%(HPLC) |
| CASNumber | 877399-52-5 |
| PubChemID | 11626560 |
| InChIKey | KTEIFNKAUNYNJU-GFCCVEGCSA-N |
| Smiles | ClC1=[C@@]([C@H](OC2=C(N)N=CC(C3=CN(C4CCNCC4)N=C3)=C2)C)C(Cl)=CC=C1F |
Thetechnicaldataprovidedaboveisforguidanceonly.ForbatchspecificdatarefertotheCertificateofAnalysis.
AllTocrisproductsareintendedforlaboratoryresearchuseonly.
SolubilityData
| Solvent | MaxConc.mg/mL | MaxConc.mM | |
|---|---|---|---|
| Solubility | |||
| 2eq.HCl | 45.03 | 100 | |
| DMSO | 4.5 | 10 | |
| ethanol | 4.5 | 10 |
PreparingStockSolutions
Thefollowingdataisbasedontheproductmolecularweight450.34.Batchspecificmolecularweightsmayvaryfrombatchtobatchduetosolventofhydration,whichwillaffectthesolventvolumesrequiredtopreparestocksolutions.
| Concentration/SolventVolume/Mass | 1mg | 5mg | 10mg |
|---|---|---|---|
| 1mM | 2.22mL | 11.1mL | 22.21mL |
| 5mM | 0.44mL | 2.22mL | 4.44mL |
| 10mM | 0.22mL | 1.11mL | 2.22mL |
| 50mM | 0.04mL | 0.22mL | 0.44mL |
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