ChemicalName: | N-cyclopropyl-4-(thiophen-3-yl)-3-(3-(3-(trifluoromethyl)phenyl)ureido)benzenesulfonamide |
MolecularWeight: | 481.51 |
Formula: | C21H18F3N3O3S2 |
Purity: | ≥98% |
CAS#: | 1432660-47-3 |
Solubility: | DMSOupto50mM |
Storage: | Powder:4oC1yearDMSO:4oC3month-20oC1year |
AGI-6780isthefirsthighlypotentandselectivesmallmoleculeinhibitorofmutantIDH2,whichbindsinanallostericmanneratthedimerinterfaceofmutantIDH2-R140Q.ItinhibitsIDH2-R140QinvitrowithanIC50~23nMandinhibits2-HGformationinhumanglioblastomaU87andTF-1cellsexpressingIDH2-R140QwithIC50<20nM.AGI-6780canreversethedifferentiationblockadeinTF-1cellsconferredbyIDH2-R140Q,andinduceblastdifferentiationinprimaryhumanIDH2-R140QAMLpatientsamples.Itprovidesproof-of-conceptthatinhibitorstargetingmutantIDH2-R140Qcouldhavepotentialapplicationsasadifferentiationtherapyforcancer.
HowtoUse:
Invitro:AGI-6780wassuggestedtobeusedat1-5µMfinalconcentrationinvitro.
Invivo:n/a
Reference:
- 1.FangWang,etal.TargetedInhibitionofMutantIDH2inLeukemiaCellsInducesCellularDifferentiation.(2013)Science.340(6132):622-6.
Productsareforresearchuseonly.Notforhumanuse.