BiologicalActivity
Selectiveinhibitorofpolo-likekinase1(PLK1)andpolo-likekinase3(PLK3)(IC50valuesare2.2and9.1nMrespectively).Displays>100-foldselectivityover~30otherkinasestestedincludingcdk1andcdk2.Inhibitsproliferationofmosttumorcellsinvitroandisselectiveovernormaldiploidfibroblasts.
LicensingInformation
SoldforresearchpurposesunderagreementfromGlaxoSmithKline
CompoundLibraries
GW843682XisalsoofferedaspartoftheTocriscreenPlusandTocriscreenKinaseInhibitorToolboxI.FindoutmoreaboutcompoundlibrariesavailablefromTocris.
TechnicalData
| M.Wt | 477.46 |
| Formula | C22H18F3N3O4S |
| Storage | Desiccateat+4°C |
| Purity | ≥98%(HPLC) |
| CASNumber | 660868-91-7 |
| PubChemID | 9826308 |
| InChIKey | JSKUWFIZUALZLX-UHFFFAOYSA-N |
| Smiles | O=C(N)C(S3)=C(OCC4=CC=CC=C4C(F)(F)F)C=C3N2C1=CC(OC)=C(OC)C=C1N=C2 |
Thetechnicaldataprovidedaboveisforguidanceonly.ForbatchspecificdatarefertotheCertificateofAnalysis.
AllTocrisproductsareintendedforlaboratoryresearchuseonly.
SolubilityData
| Solvent | MaxConc.mg/mL | MaxConc.mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 35.81 | 75 | |
| ethanol | 2.39 | 5 |
PreparingStockSolutions
Thefollowingdataisbasedontheproductmolecularweight477.46.Batchspecificmolecularweightsmayvaryfrombatchtobatchduetosolventofhydration,whichwillaffectthesolventvolumesrequiredtopreparestocksolutions.
| Concentration/SolventVolume/Mass | 1mg | 5mg | 10mg |
|---|---|---|---|
| 1mM | 2.09mL | 10.47mL | 20.94mL |
| 5mM | 0.42mL | 2.09mL | 4.19mL |
| 10mM | 0.21mL | 1.05mL | 2.09mL |
| 50mM | 0.04mL | 0.21mL | 0.42mL |
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