BiologicalActivity
Potent,selectivecdk2inhibitor(IC50valuesare0.022,0.04,0.2,>10,>10,18and>100μMforcdk2,cdk1,cdk4,PKC,p38,PDGFRandEGFRrespectively).InhibitspRbphosphorylationcausingenhancedpRB/E2FcomplexformationandinducesG1andG2-Mcellcyclearrest.TranscriptionallydownregulatesMcl-1andhasantiproliferative,cytostaticandpro-apoptoticeffectsinvitro.
CompoundLibraries
SU9516isalsoofferedaspartoftheTocriscreenPlus.FindoutmoreaboutcompoundlibrariesavailablefromTocris.
TechnicalData
| M.Wt | 241.25 |
| Formula | C13H11N3O2 |
| Storage | Storeat+4°C |
| Purity | ≥99%(HPLC) |
| CASNumber | 377090-84-1 |
| PubChemID | 5289419 |
| InChIKey | QNUKRWAIZMBVCU-WCIBSUBMSA-N |
| Smiles | O=C2NC1=CC=C(OC)C=C1/C2=C/C3=CNC=N3 |
Thetechnicaldataprovidedaboveisforguidanceonly.ForbatchspecificdatarefertotheCertificateofAnalysis.
AllTocrisproductsareintendedforlaboratoryresearchuseonly.
SolubilityData
| Solvent | MaxConc.mg/mL | MaxConc.mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 24.12 | 100 | |
| ethanol | 4.83 | 20 |
PreparingStockSolutions
Thefollowingdataisbasedontheproductmolecularweight241.25.Batchspecificmolecularweightsmayvaryfrombatchtobatchduetosolventofhydration,whichwillaffectthesolventvolumesrequiredtopreparestocksolutions.
| Concentration/SolventVolume/Mass | 1mg | 5mg | 10mg |
|---|---|---|---|
| 1mM | 4.15mL | 20.73mL | 41.45mL |
| 5mM | 0.83mL | 4.15mL | 8.29mL |
| 10mM | 0.41mL | 2.07mL | 4.15mL |
| 50mM | 0.08mL | 0.41mL | 0.83mL |

