| MolecularWeight: | 473.38 |
| Formula: | C19H17F6N7O |
| Purity: | ≥98% |
| CAS#: | 1446502-11-9 |
| Solubility: | DMSOupto50mM |
| ChemicalName: | 2-methyl-1-((4-(6-(trifluoromethyl)pyridin-2-yl)-6-((2-(trifluoromethyl)pyridin-4-yl)amino)-1,3,5-triazin-2-yl)amino)propan-2-ol |
| Storage: | Powder:4oC1year.DMSO:4oC3month;-20oC1year. |
BIOLOGicalActivity:AG-221(Enasidenib)isapotentandselectiveinhibitorofIDH2R140QmutantwithIC50~16nM.Itcanreduceintracellularandextracellularlevelsof2-HGinTF-1/IDH2(R140Q)mutantcellsinadose-dependentmanner.ItcanreduceIDH2(R140Q)-inducedGM-CSF-independentgrowth,reducehistonehypermethylationassociatedwithelevatedlevelsof2-HG.InvivotreatmentwithAG-221inU87MGIDH2(R140Q)tumorxenograftmodelleadtoareductionintumor2-HGconcentration.AdosedependentdecreaseinleukemiaandevidenceofnormaldifferentiationwasseeninAG-221treatedNOD/SCIDmiceengraftedwithAMM7577-P2cells.NowthedrugisinclinicaltrialsforIDH2mutant-positiveAML.HowtoUse:Invitro:AG-221wasusedat1µMinvitroandcellularassays.Invivo:AG-221wasdosedorallytomicebearingIDH2mutanttumorsat5-50mg/Kgonceperday.Reference:
- 1.http://investor.agios.com/phoenix.zhtml?c=251862&p=irol-publications
- 2.Chong-HuiGu,etal.Crystallineformsoftherapeuticallyactivecompoundsandusethereof.(2015)PCTWO2015018060
AG-221_spec.pdfAG-221_MSDS.pdfProductsareforresearchuseonly.Notforhumanuse.
