Name: CPI-169
Price: 274.00 USD

- Overview
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    Background
    
    CPI-169 is a novel, small molecule and potent inhibitor of enhancer of zeste homolog 2 (EZH2) with an IC50 value of <1nM for polycomb repressive complex 2 (PRC2) [1].CPI-169 has been found to be a potent EZH2 inhibitor with an IC50 value of <1nM for polycomb repressive complex 2 (PRC2). In addition, CPI-169 has been reported to reduce cellular levels of histone H3 on lysine 27(H3K27) with an EC50 value of 70nM. Moreover, CPI-169 has been exhibited to trigger cell cycle arrest and apoptosis in cells. Apart from these, treatment the inhibitor at 200mpk twice daily, CPI-169 has been noted to have a well tolerated in mice with no observed toxic effect or body weight loss [1].
    
    [1] Vidya Balasubramanian, Priya Iyer, Shilpi Arora, Patrick Troyer, Emmanuel Normant. Constellation Pharmaceuticals, Cambridge, MA. CPI-169, a novel and potent EZH2 inhibitor, synergizes with CHOP in vivo and achieves complete regression in lymphoma xenograft models
- Properties
  - Alternative Name
    
    (R,Z)-1-(1-(1-(ethylsulfonyl)piperidin-4-yl)ethyl)-N-((2-hydroxy-4-methoxy-6-methylpyridin-3-yl)methyl)-2-methyl-1H-indole-3-carbimidic acid
    
    CAS Number
    
    1450655-76-1
    
    Molecular Formula
    
    C27H36N4O5S
    
    Molecular Weight
    
    528.66
    
    Appearance
    
    A solid
    
    Purity
    
    99.30%
    
    Solubility
    
    ≥26.45 mg/mL in DMSO; insoluble in H2O; ≥2.18 mg/mL in EtOH with gentle warming and ultrasonic
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only
- Reference
  - 1. Bolouri H, Young M, et al. "Integrative network modeling reveals mechanisms underlying T cell exhaustion." ci Rep. 2020;10(1):1915. PMID:32024856
    2. Hamid Bolouri, Mary Young, et al. "Integrative network modeling reveals mechanisms underlying T cell exhaustion." bioRxiv. 2019 March 19.

CPI-169

CPI-169

Background

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