BiologicalActivity
Potent,ATP-competitiveinhibitorofmitogen-activatedproteinkinase(MAPK)-activatedproteinkinase-2(MK2)(IC50=5.2nM;Ki=3nM).Inhibitstumornecrosisfactorα(TNFα)productioninU937monocyticcellsandperipheralbloodmononuclearcells(PBMCs)(IC50=160nM);exhibitsoralefficacyinacuteandchronicinflammatorymodels.
LicensingInformation
SoldforresearchpurposesunderagreementfromPfizerInc.
ExternalPortalInformation
Chemicalprobes.orgisaportalthatoffersindependentguidanceontheselectionand/orapplicationofsmallmoleculesforresearch.TheuseofPF3644022isreviewedonthechemicalprobeswebsite..
TechnicalData
| M.Wt | 374.46 |
| Formula | C21H18N4OS |
| Storage | Storeat+4°C |
| Purity | ≥98%(HPLC) |
| CASNumber | 1276121-88-0 |
| PubChemID | 44631903 |
| InChIKey | CMWRPDHVGMHLSZ-GFCCVEGCSA-N |
| Smiles | O=C(N[C@H](C)CN4)C3=C4C1=C(S3)C=CC2=C1C=CC(C5=CC=C(C)N=C5)=N2 |
Thetechnicaldataprovidedaboveisforguidanceonly.ForbatchspecificdatarefertotheCertificateofAnalysis.
AllTocrisproductsareintendedforlaboratoryresearchuseonly.
SolubilityData
| Solvent | MaxConc.mg/mL | MaxConc.mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 14.98 | 40 |
PreparingStockSolutions
Thefollowingdataisbasedontheproductmolecularweight374.46.Batchspecificmolecularweightsmayvaryfrombatchtobatchduetosolventofhydration,whichwillaffectthesolventvolumesrequiredtopreparestocksolutions.
| Concentration/SolventVolume/Mass | 1mg | 5mg | 10mg |
|---|---|---|---|
| 1mM | 2.67mL | 13.35mL | 26.71mL |
| 5mM | 0.53mL | 2.67mL | 5.34mL |
| 10mM | 0.27mL | 1.34mL | 2.67mL |
| 50mM | 0.05mL | 0.27mL | 0.53mL |
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