BiologicalActivity
Potent3-phosphoinositide-dependentproteinkinase(PDPK1)inhibitor(IC50~10nM).ExhibitsnoeffectonotherkinasesincludingAurora,ROCK,p38MAPKandPI3-K.SuppressesT-loopphosphorylationandsubsequentactivationofPDK1substratesS6K1,SGKandRSKinvitro;exhibitslimitedinhibitoryeffectonAktactivation.DelaysmelanomagenesisandmetastasisinBrafV600E::Pten(-/-)mice.
LicensingInformation
SoldforresearchpurposesonlyunderagreementfromGlaxoSmithKline
ExternalPortalInformation
Chemicalprobes.orgisaportalthatoffersindependentguidanceontheselectionand/orapplicationofsmallmoleculesforresearch.TheuseofGSK2334470isreviewedonthechemicalprobeswebsite.
CompoundLibraries
GSK2334470isalsoofferedaspartoftheTocriscreenPlusandTocriscreenKinaseInhibitorToolboxI.FindoutmoreaboutcompoundlibrariesavailablefromTocris.
TechnicalData
| M.Wt | 462.59 |
| Formula | C25H34N8O |
| Storage | Storeat+4°C |
| Purity | ≥98%(HPLC) |
| CASNumber | 1227911-45-6 |
| PubChemID | 46215815 |
| InChIKey | QLPHOXTXAKOFMU-WBVHZDCISA-N |
| Smiles | C[C@H]1N(C3=NC(NC)=NC(C4=CC(NN=C5N)=C5C=C4)=C3)C[C@@H]([C@](NC2CCCCC2)=O)CC1 |
Thetechnicaldataprovidedaboveisforguidanceonly.ForbatchspecificdatarefertotheCertificateofAnalysis.
AllTocrisproductsareintendedforlaboratoryresearchuseonly.
SolubilityData
| Solvent | MaxConc.mg/mL | MaxConc.mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 46.26 | 100 | |
| ethanol | 46.26 | 100 |
PreparingStockSolutions
Thefollowingdataisbasedontheproductmolecularweight462.59.Batchspecificmolecularweightsmayvaryfrombatchtobatchduetosolventofhydration,whichwillaffectthesolventvolumesrequiredtopreparestocksolutions.
| Concentration/SolventVolume/Mass | 1mg | 5mg | 10mg |
|---|---|---|---|
| 1mM | 2.16mL | 10.81mL | 21.62mL |
| 5mM | 0.43mL | 2.16mL | 4.32mL |
| 10mM | 0.22mL | 1.08mL | 2.16mL |
| 50mM | 0.04mL | 0.22mL | 0.43mL |
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ProductDatasheets
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