Name: CCT251545 analogue, Compound 51
Price: 528.00 USD

- Overview
  - Please contact us at for specific academic pricing.
    
    Background
    
    CCT251545 analogue, Compound 51 is a potent and selective CDK8/19 inhibitor with IC50 values of 5.1 nM and 5.6 nM, respectively [1]. Mediator complex-associated kinases CDK8 and CDK19 are involved in the regulation of multiple transcription pathways. CDK8 plays as an oncogene in gastric and colorectal cancers through activation of WNT signaling [1]. CCT251545 analogue, Compound 51 is a potent and selective CDK8/19 inhibitor. In SW620 human colorectal carcinoma cells harbouring activating APC-mutation, Compound 51 inhibited phospho-STAT1SER727 with IC50 value of 17.9 nM, a biomarker of CDK8 inhibition [1]. In vivo mouse and rat PK experiments, Compound 51 demonstrated medium in vivo clearance and Vd but low bioavailability in mice. In a SW620 colorectal carcinoma human tumor xenograft model, Compound 51 (5 mg/kg po dose) inhibited phospho-STAT1SER727 in a time-dependent way. Compound 51 is an advanced chemical tool to further explore the efficacy, safety and tolerability of dual CDK8/19 ligands [1].
- Properties
  - Alternative Name
    
    (5-amino-8-(4-(1-methyl-1H-pyrazol-4-yl)phenyl)-1,6-naphthyridin-2-yl)(3-methoxyazetidin-1-yl)methanone
    
    Molecular Formula
    
    C23H22N6O2
    
    Molecular Weight
    
    414.46
    
    Appearance
    
    A solid
    
    Purity
    
    98.39%
    
    Solubility
    
    ≥20.7 mg/mL in DMSO with gentle warming; insoluble in H2O; insoluble in EtOH
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only

CCT251545 analogue, Compound 51

CCT251545 analogue, Compound 51

Background

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