10074-G5

- Overview
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    Background
    
    10074-G5 is a c-Myc inhibitor [1].c-Myc is a bHLH-ZIP transcription factor involved in cell cycle progression, cellular growth and metabolism, differentiation, and apoptosis. Overexpression of c-Myc has been identified in numerous cancers, including prostate, pancreatic, lung, breast, and colon cancers, B-cell lymphoma, and leukemias. Alterations in c-Myc have been associated with cancer aggressiveness and poor treatment prognosis. Inhibition of c-Myc is an attractive pharmacological approach in the development of new anticancer treatments. Inactivation of c-Myc rapidly results in cell-cycle arrest, apoptosis, tumor vascular degeneration, redifferentiation of tumor cells, and ultimately tumor regression [1].The IC50 values of 10074-G5 against Daudi cells and HL-60 cells were 15.6 ± 1.5 μM and 13.5 ± 2.1 μM, respectively. 10074-G5 (10 μM) inhibited c-Myc/Max dimerization and decreased total c-Myc protein expression. In C.B-17 SCID mice bearing Daudi xenografts, treatment with 10074-G5, (20 mg/kg i.v., for 10 consecutive days) significantly inhibited tumor growth with no effects on body weight.
    
    [1] Clausen D M, Guo J, Parise R A, et al. In vitro cytotoxicity and in vivo efficacy, pharmacokinetics, and metabolism of 10074-G5, a novel small-molecule inhibitor of c-Myc/Max dimerization[J]. Journal of Pharmacology and Experimental Therapeutics, 2010, 335(3): 715-727.
- Properties
  - Alternative Name
    
    N-[1,1'-biphenyl]-2-yl-7-nitro-2,1,3-benzoxadiazol-4-amine
    
    CAS Number
    
    413611-93-5
    
    Molecular Formula
    
    C18H12N4O3
    
    Molecular Weight
    
    332.3
    
    Appearance
    
    A crystalline solid
    
    Purity
    
    98.00%
    
    Solubility
    
    ≥37.9 mg/mL in DMSO; ≥3.53 mg/mL in EtOH with ultrasonic; insoluble in H2O
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only

10074-G5

Background

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