Name: THZ2
Price: 880.00 USD

- Overview
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    Background
    
    THZ2 is a potent and selective CDK7 inhibitor (IC50=13.9 nM).
    Cyclin-dependent kinase (CDK) is a group of serine/threonine kinases. It is activated by binding to cyclin and participates in the regulation of cell cycle.
    THZ2 selectively targets CDK7 and potently blocks the proliferation of triple-negative breast cancer (TNBC) cells and induces apoptotic cell death without causing alteration in cell cycle. The low nanomolar dose of THZ2 also inhibits the clonogenic growth of TNBC cells with IC50 of 10 nM.
    THZ2 is well tolerant in mice as 10 mg/kg intraperitoneal treatment of THZ2 twice daily does not cause weight loss or behavioral changes. THZ2 treatment also significantly reduces the tumor growth rate mice. In addition, both acute (50 hr) or chronic (25 days) exposure to THZ markedly decreases CTD phosphorylation of RNAPII at all three phosphorylation sites as indication of CDk7 being efficiently targeted.
- Properties
  - Alternative Name
    
    CDK7-IN-1; (Z)-N-(3-((5-chloro-4-(1H-indol-3-yl)pyrimidin-2-yl)amino)phenyl)-3-((Z)-((E)-4-(dimethylamino)-1-hydroxybut-2-en-1-ylidene)amino)benzimidic acid
    
    CAS Number
    
    1604810-84-5
    
    Molecular Formula
    
    C31H28ClN7O2
    
    Molecular Weight
    
    566.05
    
    Appearance
    
    A solid
    
    Purity
    
    98.04%
    
    Solubility
    
    ≥28.3 mg/mL in DMSO; insoluble in H2O; ≥2.96 mg/mL in EtOH with gentle warming and ultrasonic
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only
- Reference
  - 1. Huang JR, Qin WM, et al. "Cyclin-dependent kinase 7 inhibitor THZ2 inhibits the growth of human gastric cancer in vitro and in vivo." Am J Transl Res. 2018 Nov 15;10(11):3664-3676. PMID:30662617

THZ2

THZ2

Background

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