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首页-小分子抑制剂&激动剂-Metabolic Enzyme/Protease-Isocitrate Dehydrogenase (IDH)-AGI-14100
AGI-14100

Chemical Structure : AGI-14100

CAS No.: 1448346-43-7

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AGI-14100 (AGI14100)

货号: PC-35206Not For Human Use, Lab Use Only.

AGI-14100 (AGI14100) is a novel potent and selective, orally available IDH1 mutant inhibitor, inhibits cell proliferation (human cell lines transfected with IDH1 R132H) with IC50 values of 0.76 nM (HT-1080), 0.74 nM (U87-MG) and 1.75 nM (TF1).

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

    生物&药学活性

    AGI-14100 (AGI14100) is a novel potent and selective, orally available IDH1 mutant inhibitor, inhibits cell proliferation (human cell lines transfected with IDH1 R132H) with IC50 values of 0.76 nM (HT-1080), 0.74 nM (U87-MG) and 1.75 nM (TF1).
    AGI-14100 can specifically induce cellular differentiation in AML patient samples with mutant IDH1 ex vivo.
    AGI-14100 significantly reduces the leukemic blast burden in the peripheral blood in xenograft model with a primary human IDH1 R132H/FLT3-ITD tumor.

    物理化学性质&存储条件

    分子量 599.971
    分子式 C29H22ClF4N5O3
    外观性状 Solid
    CAS No.
    储存条件
    固体粉末
    -20 °C 12 个月; 4°C 6 个月
    配置液
    -80 °C 6 个月; -20°C 6 个月
    Shipping
    Solubility

    10 mM in DMSO
    Chemical Name/SMILES

    (S)-N-((S)-1-(2-chlorophenyl)-2-((3,3-difluorocyclobutyl)amino)-2-oxoethyl)-1-(4-cyanopyridin-2-yl)-N-(3,5-difluorophenyl)-5-oxopyrrolidine-2-carboxamide

    参考文献

    1. Ma T, et al. J Med Chem. 2018 Jun 18. doi: 10.1021/acs.jmedchem.8b00159.
    2. Kate Ellwood-Yen, et al. Abstract 1194: IDH1 mutant inhibitor induces cellular differentiation and offers a combination benefit with Ara-C in a primary human Idh1 mutant AML xenograft model. AACR Annual Meeting 2014; April 5-9, 2014; San Diego, CA.

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