BiologicalActivity
ERK5(BMK1)andBRD4inhibitor(Kdvaluesare80and190nM,respectively).AlsoinhibitsDCAMKL2,PLK4andTNK1(Kdvaluesare190,600and890nM).Blocksgrowthfactor-inducedactivationofcellularBMK1andreducesBMK1activityininvitrokinaseassays.AlsoreducesBMK1-dependenttransactivatingactivityofMEF2C.Inhibitsproliferationinavarietyofcancercelllines;blockstumorcellproliferationandtumor-associatedangiogenesis.
LicensingInformation
SoldunderlicensefromtheDana-FarberCancerInstitute.
ExternalPortalInformation
Chemicalprobes.orgisaportalthatoffersindependentguidanceontheselectionand/orapplicationofsmallmoleculesforresearch.TheuseofXMD8-92isreviewedonthechemicalprobeswebsite.
CompoundLibraries
XMD8-92isalsoofferedaspartoftheTocriscreenPlusandTocriscreenKinaseInhibitorToolboxI.FindoutmoreaboutcompoundlibrariesavailablefromTocris.
TechnicalData
| M.Wt | 474.55 |
| Formula | C26H30N6O3 |
| Storage | StoreatRT |
| Purity | ≥98%(HPLC) |
| CASNumber | 1234480-50-2 |
| PubChemID | 46843772 |
| InChIKey | QAPAJIZPZGWAND-UHFFFAOYSA-N |
| Smiles | O=C2C3=C(C=CC=C3)N(C)C1=NC(NC4=C(OCC)C=C(N5CCC(O)CC5)C=C4)=NC=C1N2C |
Thetechnicaldataprovidedaboveisforguidanceonly.ForbatchspecificdatarefertotheCertificateofAnalysis.
AllTocrisproductsareintendedforlaboratoryresearchuseonly.
SolubilityData
| Solvent | MaxConc.mg/mL | MaxConc.mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 18.98 | 40 |
PreparingStockSolutions
Thefollowingdataisbasedontheproductmolecularweight474.55.Batchspecificmolecularweightsmayvaryfrombatchtobatchduetosolventofhydration,whichwillaffectthesolventvolumesrequiredtopreparestocksolutions.
| Concentration/SolventVolume/Mass | 1mg | 5mg | 10mg |
|---|---|---|---|
| 1mM | 2.11mL | 10.54mL | 21.07mL |
| 5mM | 0.42mL | 2.11mL | 4.21mL |
| 10mM | 0.21mL | 1.05mL | 2.11mL |
| 50mM | 0.04mL | 0.21mL | 0.42mL |

