Name: AG-120
Price: 252.00 USD

- Overview
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    Background
    
    IC50: < 100 nMAG-120 is an IDH1 inhibitor.Isocitrate dehydrogenase (IDH) is a metabolic enzyme interconverting isocitrate and α-ketoglutarate (α-KG), but cancer-associated mutations of IDH1 and IDH2 confer a neomorphic activity, which allows reduction of α-KG to the oncometabolite 2-HG.In vitro: TF-1 cells or primary human AML patient samples expressing mutant IDH1 were treated with AG-120, and the results showed that in TF-1 IDH1-R132H cells, AG-120 was able to decrease the intracellular 2-HG levels, inhibit growth factor independent proliferation and restore erythropoietin-induced differentiation [1]. Ex vivo: Previous ex-vivo study showed that the pharmacological inhibition of mutant IDH1 enzyme with AG-120 in primary human blast cells led to an effective way to lower intracellular 2-HG levels and induced myeloid differentiation [1]. Clinical trial: In a phase I clinical trial, 62 patients with advanced IDH1 mutation–positive solid tumors were treated with single agent AG-120 orally once a day. Results showed that 7 of 11 patients with IDH1 mutant–positive chondrosarcoma had stable disease; 1 out of 20 patients with IDH1 mutant–positive IHCC had a partial response and 11 patients had SD; and one out of four patients with other IDH1 mutant–positive solid tumors had SD [2].
    
    [1] Erica Hansen et al. AG-120, an Oral, Selective, First-in-Class, Potent Inhibitor of Mutant IDH1, Reduces Intracellular 2HG and Induces Cellular Differentiation in TF-1 R132H Cells and Primary Human IDH1 Mutant AML Patient Samples Treated Ex Vivo. Blood 2014 124:3734.
    [2] http://www. aacr.org/Newsroom/Pages/News-Release-Detail.aspx ItemID=789#.WLAUOm997IU
- Properties
  - Alternative Name
    
    (S)-N-((S)-1-(2-chlorophenyl)-2-((3,3-difluorocyclobutyl)amino)-2-oxoethyl)-1-(4-cyanopyridin-2-yl)-N-(5-fluoropyridin-3-yl)-5-oxopyrrolidine-2-carboxamide
    
    CAS Number
    
    1448347-49-6
    
    Molecular Formula
    
    C28H22ClF3N6O3
    
    Molecular Weight
    
    582.96
    
    Appearance
    
    A solid
    
    Purity
    
    98.00%
    
    Solubility
    
    ≥58.3 mg/mL in DMSO; insoluble in H2O; ≥63.3 mg/mL in EtOH
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only

AG-120

AG-120

Background

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