BiologicalActivity
Potent,selectivelactatedehydrogenaseA(LDHA)inhibitor(IC50valuesare1.9and14nMforLDHAandLDHBrespectively).Inhibitslactateproductioninselectedcancercelllines.ReducesglucoseuptakeandenhancesmitochondrialoxygenconsumptioninSnu398hepatocellularcarcinomacells.InhibitsproliferationandinducesapoptosisinSnu398cells.Inhibitstranscriptionofhistone2B(H2B)geneinHCT116andNCM460cells.Cellpermeable.
LicensingInformation
SoldforresearchpurposesunderagreementfromGlaxoSmithKline.
CompoundLibraries
GSK2837808AisalsoofferedaspartoftheTocriscreenPlus.FindoutmoreaboutcompoundlibrariesavailablefromTocris.
TechnicalData
| M.Wt | 649.62 |
| Formula | C31H25F2N5O7S |
| Storage | Storeat-20°C |
| Purity | ≥98%(HPLC) |
| CASNumber | 1445879-21-9 |
| PubChemID | 71533725 |
| InChIKey | RZBCPMYJIARMGV-UHFFFAOYSA-N |
| Smiles | O=S(C2=C(NC3=CC(OC5=CC(F)=CC(F)=C5)=CC(C(O)=O)=C3)C1=CC=C(C6=CN=C(OC)N=C6OC)C=C1N=C2)(NC4CC4)=O |
Thetechnicaldataprovidedaboveisforguidanceonly.ForbatchspecificdatarefertotheCertificateofAnalysis.
AllTocrisproductsareintendedforlaboratoryresearchuseonly.
SolubilityData
| Solvent | MaxConc.mg/mL | MaxConc.mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 64.96 | 100 |
PreparingStockSolutions
Thefollowingdataisbasedontheproductmolecularweight649.62.Batchspecificmolecularweightsmayvaryfrombatchtobatchduetosolventofhydration,whichwillaffectthesolventvolumesrequiredtopreparestocksolutions.
| Concentration/SolventVolume/Mass | 1mg | 5mg | 10mg |
|---|---|---|---|
| 1mM | 1.54mL | 7.7mL | 15.39mL |
| 5mM | 0.31mL | 1.54mL | 3.08mL |
| 10mM | 0.15mL | 0.77mL | 1.54mL |
| 50mM | 0.03mL | 0.15mL | 0.31mL |
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