BiologicalActivity
PotentATP-competitivePDGFRandVEGFRinhibitor(Ki=5and6nM,respectively);inhibitsphosphorylationofc-KitandsuppressesthegrowthofmastcelllinesexpressingmutantKit,inducingcellcyclearrestandapoptosis.AlsoinhibitsFGFR1(Ki=0.5μM).Effectiveinvivo.
LicensingInformation
SoldforresearchpurposesunderagreementfromPfizer.
TechnicalData
| M.Wt | 396.46 |
| Formula | C22H25FN4O2 |
| Storage | Storeat-20°C |
| Purity | ≥98%(HPLC) |
| CASNumber | 356068-94-5 |
| PubChemID | 5329106 |
| InChIKey | SRSGVKWWVXWSJT-ATVHPVEESA-N |
| Smiles | O=C2NC1=CC=C(F)C=C1/C2=C/C3=C(C)C(C(NCCN4CCCC4)=O)=C(C)N3 |
Thetechnicaldataprovidedaboveisforguidanceonly.ForbatchspecificdatarefertotheCertificateofAnalysis.
AllTocrisproductsareintendedforlaboratoryresearchuseonly.
SolubilityData
| Solvent | MaxConc.mg/mL | MaxConc.mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 3.96 | 10mMwithgentlewarming |
PreparingStockSolutions
Thefollowingdataisbasedontheproductmolecularweight396.46.Batchspecificmolecularweightsmayvaryfrombatchtobatchduetosolventofhydration,whichwillaffectthesolventvolumesrequiredtopreparestocksolutions.
| Concentration/SolventVolume/Mass | 1mg | 5mg | 10mg |
|---|---|---|---|
| 1mM | 2.52mL | 12.61mL | 25.22mL |
| 5mM | 0.5mL | 2.52mL | 5.04mL |
| 10mM | 0.25mL | 1.26mL | 2.52mL |
| 50mM | 0.05mL | 0.25mL | 0.5mL |
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