AGI-6780, Mutant IDH2 Inhibitor


Catalog No. size PriceQuantity
M60105-2D 10 mM DMSO (0.415 mL) $109
M60105-2S 2 mg solid $109
M60105-10S 10 mg solid $441

Description

Product Information
Chemical Name: N-cyclopropyl-4-(thiophen-3-yl)-3-(3-(3-(trifluoromethyl)phenyl)ureido)benzenesulfonamide
Molecular Weight: 481.51
Formula: C21H18F3N3O3S2
Purity: ≥98%
CAS#: 1432660-47-3
Solubility: DMSO up to 50 mM
Storage: Powder: 4oC 1 year DMSO: 4oC 3 month -20oC 1 year

 



Biological Activity:

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:

  1. Fang Wang, et al. Targeted Inhibition of Mutant IDH2 in Leukemia Cells Induces Cellular Differentiation. (2013) Science. 340(6132):622-6.



Products are for research use only. Not for human use.

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