BiologicalActivity
PotentandselectiveNUAK1inhibitor(IC50=100nM).Exhibitsnosignificantinhibitionagainstapanelof139kinases,includingtenAMPKfamilymembers.InhibitsNUAK1-mediatedMYPT1phosphorylation.AlsoinhibitscellproliferationinU2OScellsinvitro,toasimilarextentasNUAK1knockdownmodels.
LicensingInformation
SoldunderlicensefromDana-FarberCancerInstitute
CompoundLibraries
HTH01-015isalsoofferedaspartoftheTocriscreenPlusandTocriscreenKinaseInhibitorToolboxII.FindoutmoreaboutcompoundlibrariesavailablefromTocris.
TechnicalData
| M.Wt | 468.55 |
| Formula | C26H28N8O |
| Storage | Storeat-20°C |
| Purity | ≥98%(HPLC) |
| CASNumber | 1613724-42-7 |
| PubChemID | 78357766 |
| InChIKey | CHSDJDLAKKAWCI-UHFFFAOYSA-N |
| Smiles | O=C1N(C)C2=C(N=C(NC3=CN(C4CCNCC4)N=C3)N=C2C)N(C)C5=CC6=CC=CC=C6C=C51 |
Thetechnicaldataprovidedaboveisforguidanceonly.ForbatchspecificdatarefertotheCertificateofAnalysis.
AllTocrisproductsareintendedforlaboratoryresearchuseonly.
SolubilityData
| Solvent | MaxConc.mg/mL | MaxConc.mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 46.85 | 100 | |
| ethanol | 46.85 | 100 |
PreparingStockSolutions
Thefollowingdataisbasedontheproductmolecularweight468.55.Batchspecificmolecularweightsmayvaryfrombatchtobatchduetosolventofhydration,whichwillaffectthesolventvolumesrequiredtopreparestocksolutions.
| Concentration/SolventVolume/Mass | 1mg | 5mg | 10mg |
|---|---|---|---|
| 1mM | 2.13mL | 10.67mL | 21.34mL |
| 5mM | 0.43mL | 2.13mL | 4.27mL |
| 10mM | 0.21mL | 1.07mL | 2.13mL |
| 50mM | 0.04mL | 0.21mL | 0.43mL |
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