BiologicalActivity
PotentJAK2inhibitor(IC50=0.48nM).Exhibits>20-foldselectivityforJAK2overTYK2,JAK3andJAK1(IC50valuesare10.8,18.7and31.6nM,respectively).InhibitsproliferationandinducesapoptosisofJAK2V617F-bearingacutemyeloidleukemiacellsinvitroandinvivo.Alsoinhibitserythropoietin-inducedpolycythemia.Orallybioavailable.
TechnicalData
| M.Wt | 599.94 |
| Formula | C27H28F2N6O.3HCl |
| Storage | Storeat+4°C |
| Purity | ≥98%(HPLC) |
| Smiles | FC1=C(CN2CCOCC2)C(F)=CC(C3=C4C(N=CC(C5=CN(C6CCNCC6)N=C5)=N4)=CC=C3)=C1.Cl.Cl.Cl |
Thetechnicaldataprovidedaboveisforguidanceonly.ForbatchspecificdatarefertotheCertificateofAnalysis.
AllTocrisproductsareintendedforlaboratoryresearchuseonly.
SolubilityData
| Solvent | MaxConc.mg/mL | MaxConc.mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 30 | 50 | |
| water | 59.99 | 100 |
PreparingStockSolutions
Thefollowingdataisbasedontheproductmolecularweight599.94.Batchspecificmolecularweightsmayvaryfrombatchtobatchduetosolventofhydration,whichwillaffectthesolventvolumesrequiredtopreparestocksolutions.
| Concentration/SolventVolume/Mass | 1mg | 5mg | 10mg |
|---|---|---|---|
| 1mM | 1.67mL | 8.33mL | 16.67mL |
| 5mM | 0.33mL | 1.67mL | 3.33mL |
| 10mM | 0.17mL | 0.83mL | 1.67mL |
| 50mM | 0.03mL | 0.17mL | 0.33mL |
MolarityCalculator
ReconstitutionCalculator
Thereconstitutioncalculatorallowsyoutoquicklycalculatethevolumeofareagenttoreconstituteyourvial.Simplyenterthemassofreagentandthetargetconcentrationandthecalculatorwilldeterminetherest.