AGI-6780 is the first highly potent and selective small molecule inhibitor of mutant IDH2, which binds in an allosteric manner at the dimer interface of mutant IDH2-R140Q. It 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.
How to Use:
In vitro: AGI-6780 was suggested to be used at 1-5 µM final concentration in vitro.
In vivo: n/a
Reference:
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