BiologicalActivity
Adam17(TACE)andMMPinhibitor(IC50valuesare3,4.7,6.6,8.4,12,26and26nMforMMP-13,MMP-2,MMP-1,ADAM17,MMP-9,MMP-7andMMP-14,respectively).SuppressesTNF-αproductioninanacuteLPS-mousemodel.Reducesseverityscoreinaninvivomodelofrheumatoidarthritis.Displaysselectivecytotoxicitytotumorcellsandcancerstemcellsinvitro.Inducestumorapoptosisinabreastcancerinvivomodel.Orallybioavailable.
LicensingInformation
SoldforresearchpurposesunderagreementfromPfizerInc
TechnicalData
| M.Wt | 398.49 |
| Formula | C17H22N2O5S2 |
| Storage | Storeat-20°C |
| Purity | ≥98%(HPLC) |
| CASNumber | 287403-39-8 |
| PubChemID | 5288615 |
| InChIKey | CVZIHNYAZLXRRS-HNNXBMFYSA-N |
| Smiles | CC1(C)SCCN(S(C2=CC=C(OCC#CC)C=C2)(=O)=O)[C@H]1C(NO)=O |
Thetechnicaldataprovidedaboveisforguidanceonly.ForbatchspecificdatarefertotheCertificateofAnalysis.
AllTocrisproductsareintendedforlaboratoryresearchuseonly.
SolubilityData
| Solvent | MaxConc.mg/mL | MaxConc.mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 39.85 | 100 | |
| ethanol | 7.97 | 20 |
PreparingStockSolutions
Thefollowingdataisbasedontheproductmolecularweight398.49.Batchspecificmolecularweightsmayvaryfrombatchtobatchduetosolventofhydration,whichwillaffectthesolventvolumesrequiredtopreparestocksolutions.
| Concentration/SolventVolume/Mass | 1mg | 5mg | 10mg |
|---|---|---|---|
| 1mM | 2.51mL | 12.55mL | 25.09mL |
| 5mM | 0.5mL | 2.51mL | 5.02mL |
| 10mM | 0.25mL | 1.25mL | 2.51mL |
| 50mM | 0.05mL | 0.25mL | 0.5mL |
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ProductDatasheets
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