BiologicalActivity
Potent,ATP-competitiveinhibitorofmammaliantargetofrapamycin(mTOR)(IC50=7nM).DisplaysselectivityformTORoverPI3-Kα(~100-fold)andPI3-Kγ(~500-fold).InhibitsphosphorylationofmTORC1andmTORC2substratesincludingS6K,SGKandAkt;blocksVEGFsecretionandHIF-1αexpression.ExhibitsantiproliferativeeffectsincancercelllinesthroughG1cellcyclearrestandselectiveapoptosis.
LicensingInformation
SoldforresearchpurposesunderagreementfromPfizerInc.
CompoundLibraries
WYE687dihydrochlorideisalsoofferedaspartoftheTocriscreenPlusandTocriscreenKinaseInhibitorToolboxII.FindoutmoreaboutcompoundlibrariesavailablefromTocris.
TechnicalData
| M.Wt | 601.53 |
| Formula | C28H32N8O3 |
| Storage | DesiccateatRT |
| Purity | ≥98%(HPLC) |
| CASNumber | 1062161-90-3 |
| PubChemID | 90488926 |
| InChIKey | ZQJPHAXLAKKXIX-UHFFFAOYSA-N |
| Smiles | O=C(OC)NC(C=C4)=CC=C4C1=NC(N3CCOCC3)=C2C(N(C5CCN(CC6=CN=CC=C6)CC5)N=C2)=N1.Cl.Cl |
Thetechnicaldataprovidedaboveisforguidanceonly.ForbatchspecificdatarefertotheCertificateofAnalysis.
AllTocrisproductsareintendedforlaboratoryresearchuseonly.
SolubilityData
| Solvent | MaxConc.mg/mL | MaxConc.mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 60.15 | 100 | |
| water | 60.15 | 100 |
PreparingStockSolutions
Thefollowingdataisbasedontheproductmolecularweight601.53.Batchspecificmolecularweightsmayvaryfrombatchtobatchduetosolventofhydration,whichwillaffectthesolventvolumesrequiredtopreparestocksolutions.
| Concentration/SolventVolume/Mass | 1mg | 5mg | 10mg |
|---|---|---|---|
| 1mM | 1.66mL | 8.31mL | 16.62mL |
| 5mM | 0.33mL | 1.66mL | 3.32mL |
| 10mM | 0.17mL | 0.83mL | 1.66mL |
| 50mM | 0.03mL | 0.17mL | 0.33mL |
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ProductDatasheets
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