Name: PTC209 HBr
Price: 292.00 USD

- Overview
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    Background
    
    PTC-209 HBr is the hydrobromide salt of PTC-209, a potent and selective BMI-1 inhibitor (IC50 = 0.5μM). It irreversibly impairs the colorectal tumor growth. [1]BMI-1 is a component of polycomb repressive complex 1 (PRC1) and act as an epigenetic chromatin modifier for a variety of genes. [1]PTC-209 inhibited both UTR-mediated reporter expression and endogenous BMI-1 expression in HCT116 (human colorectal cell) and HT1080 (human fibrosarcoma tumor cell) in a dose dependent manner. In addition, the inhibitory effect of PTC-209 was not from its cytotoxicity. PTC-209 also specifically reduced PRC1 activity. [1]Viable colorectal cancer cell samples treated with PTC-209 ex vivo were injected back to the recipient mice in vivo, the mice exhibited reduced or no tumor growth comparing with the control groups. Thus PTC-209 irreversibly impaired colorectal cancer-initiating cells. Furthermore, in contrast with the control groups, tumor volume was significantly reduced in the colorectal tumor cell transplanted mice following PTC-209 administration. [1]
    
    [1] Kreso A, van Galen P, Pedley NM, Lima-Fernandes E, Frelin C, Davis T, Cao L,Baiazitov R, Du W, Sydorenko N, Moon YC, Gibson L, Wang Y, Leung C, Iscove NN,Arrowsmith CH, Szentgyorgyi E, Gallinger S, Dick JE, O'Brien CA. Self-renewal as a therapeutic target in human colorectal cancer. Nat Med. 2014 Jan;20(1):29-36.
- Properties
  - Alternative Name
    
    N-(2,6-dibromo-4-methoxyphenyl)-4-(2-methylimidazo[1,2-a]pyrimidin-3-yl)thiazol-2-amine hydrobromide
    
    CAS Number
    
    1217022-63-3
    
    Molecular Formula
    
    C17H13Br2N5OS·HBr
    
    Molecular Weight
    
    576.10
    
    Appearance
    
    A solid
    
    Purity
    
    98.00%
    
    Solubility
    
    ≥22.9 mg/mL in DMSO with gentle warming; insoluble in EtOH; insoluble in H2O
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only