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 AGI-6780,MutantIDH2Inhibitor M60105-2s|产品详情|进口橙子视频旧款采购网




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    上海橙子视频app安卓下载生物科技公司
    Tel:400-968-7988    021-33779008
    AGI-6780,MutantIDH2Inhibitor
    品牌:Xcessbio
    货号:M60105-2s
    规格:2 mg solid
    货期:

    AGI-6780,MutantIDH2Inhibitor

    商品详情 参考文献 相关资料
    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. 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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