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 |