||Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity of AGI-6780
AGI-6780 is the first highly potent and selective small molecule inhibitor of isocitrate dehydrogenases, which binds in an allosteric manner at the dimer interface of mutant IDH2-R140Q (IC50=23 nM).
IC50 Value: 23 nM (IDH2-R140Q) 
Target: mutant IDH2-R140Q
in vitro: AGI-6780 inhibits IDH2-R140Q in vitro with an IC50 ~23 nM and inhibits 2-HG formation in human glioblastoma U87 and TF-1 cells expressing IDH2-R140Q with IC50 < 20 nM. AGI-6780 can reverse the differentiation blockade in TF-1 cells conferred by IDH2-R140Q, and induce blast differentiation in primary human IDH2-R140Q AML patient samples. It provides proof-of-concept that inhibitors targeting mutant IDH2-R140Q could have potential applications as a differentiation therapy for cancer .
in vivo: N/A
Clinical trial: Phase I Study of AG-221 in Subjects With Advanced Hematological Malignancies With an IDH2 Mutation. Phase 1
Clinical Information of AGI-6780
. Wang F, et al. Targeted inhibition of mutant IDH2 in leukemia cells induces cellular differentiation. Science. 2013 May 3;340(6132):622-6.