BiologicalActivity
PotentandselectiveallostericinhibitorofWip1phosphatase(IC50=6nM).ExhibitsselectivityforWip1over21otherphosphatases.IncreasesphosphorylationofWip1substrates,includingp53,Chk2,H2AXandATM.Attenuatestumorcellgrowthinavarietyoflymphoidcelllines.Alsoinhibitslymphomaxenograftgrowthinvivo.Orallybioavailable.
LicensingInformation
SoldforresearchpurposesonlyunderagreementfromGlaxoSmithKline
CompoundLibraries
GSK2830371isalsoofferedaspartoftheTocriscreenPlus.FindoutmoreaboutcompoundlibrariesavailablefromTocris.
TechnicalData
| M.Wt | 461.02 |
| Formula | C23H29ClN4O2S |
| Storage | Storeat-20°C |
| Purity | ≥98%(HPLC) |
| CASNumber | 1404456-53-6 |
| PubChemID | 70983932 |
| InChIKey | IVDUVEGCMXCMSO-FQEVSTJZSA-N |
| Smiles | ClC1=CC(NCC2=CC=C(C(N[C@H]([C@@](NC4CC4)=O)CC3CCCC3)=O)S2)=C(C)N=C1 |
Thetechnicaldataprovidedaboveisforguidanceonly.ForbatchspecificdatarefertotheCertificateofAnalysis.
AllTocrisproductsareintendedforlaboratoryresearchuseonly.
SolubilityData
| Solvent | MaxConc.mg/mL | MaxConc.mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 46.1 | 100 | |
| ethanol | 23.05 | 50 |
PreparingStockSolutions
Thefollowingdataisbasedontheproductmolecularweight461.02.Batchspecificmolecularweightsmayvaryfrombatchtobatchduetosolventofhydration,whichwillaffectthesolventvolumesrequiredtopreparestocksolutions.
| Concentration/SolventVolume/Mass | 1mg | 5mg | 10mg |
|---|---|---|---|
| 1mM | 2.17mL | 10.85mL | 21.69mL |
| 5mM | 0.43mL | 2.17mL | 4.34mL |
| 10mM | 0.22mL | 1.08mL | 2.17mL |
| 50mM | 0.04mL | 0.22mL | 0.43mL |
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