BiologicalActivity
PotentandselectiveSAM-competitiveEZH2inhibitor(IC50=4mM).Exhibits>60foldselectivityforEZH2overEZH1andarangeofothermethyltransferases.Inhibitsproliferationofprostatecancercelllinesinvitro.
LicensingInformation
ThisprobeissuppliedinconjunctionwiththeStructuralGenomicsConsortium.Forfurthercharacterizationdetails,pleasevisittheGSK343probesummaryontheSGCwebsite.
TechnicalData
| M.Wt | 541.69 |
| Formula | C31H39N7O2 |
| Storage | Storeat-20°C |
| Purity | ≥98%(HPLC) |
| CASNumber | 1346704-33-3 |
| PubChemID | 71268957 |
| InChIKey | ULNXAWLQFZMIHX-UHFFFAOYSA-N |
| Smiles | CCCC1=C(C(NC(C)=C1)=O)CNC(C2=C3C=NN(C3=CC(C4=CC=NC(N5CCN(CC5)C)=C4)=C2)C(C)C)=O |
Thetechnicaldataprovidedaboveisforguidanceonly.ForbatchspecificdatarefertotheCertificateofAnalysis.
AllTocrisproductsareintendedforlaboratoryresearchuseonly.
SolubilityData
| Solvent | MaxConc.mg/mL | MaxConc.mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 10.83 | 20mMwithgentlewarming |
PreparingStockSolutions
Thefollowingdataisbasedontheproductmolecularweight541.69.Batchspecificmolecularweightsmayvaryfrombatchtobatchduetosolventofhydration,whichwillaffectthesolventvolumesrequiredtopreparestocksolutions.
| Concentration/SolventVolume/Mass | 1mg | 5mg | 10mg |
|---|---|---|---|
| 1mM | 1.85mL | 9.23mL | 18.46mL |
| 5mM | 0.37mL | 1.85mL | 3.69mL |
| 10mM | 0.18mL | 0.92mL | 1.85mL |
| 50mM | 0.04mL | 0.18mL | 0.37mL |
MolarityCalculator
ReconstitutionCalculator
Thereconstitutioncalculatorallowsyoutoquicklycalculatethevolumeofareagenttoreconstituteyourvial.Simplyenterthemassofreagentandthetargetconcentrationandthecalculatorwilldeterminetherest.
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