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KI3762AGI67805 mg$190

Chemical Characteristic

Product NameAGI6780
CAS No.1432660-47-3
Molecular Weight 481.51
FormulaC21H18F3N3O3S2
Chemical NameBenzenesulfonamide, N-cyclopropyl-4-(3-thienyl)-3-[[[[3-(trifluoromethyl)phenyl]amino]carbonyl]amino]-
Smilesc1(cc(c(cc1)c1cscc1)NC(=O)Nc1cc(ccc1)C(F)(F)F)S(=O)(=O)NC1CC1
Chemical Structure

Biological activities

AGI6780 inhibits the tumor-associated mutant IDH2/R140Q potently and selectively(IC50=23 nM). It binds in an allosteric manner at the dimer interface of mutant IDH2-R140Q. In vitro, AGI-6780 was suggested to be used at a final concentration of 1-5 ?M.TF-1 erythroleukemia and primary human acute myelogenous leukemia cells were induced differentiation by AGI6780. It provides proof-of-concept that inhibitors targeting mutant IDH2-R140Q could have potential applications as a differentiation therapy for cancer. [1]

References

[1] Wang F, Travins J, DeLaBarre B, et al. Targeted Inhibition of Mutant IDH2 in Leukemia Cells Induces Cellular Differentiation. Science. 2013,340(6132):622-626.

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