AZD-5597

- Overview
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    Background
    
    AZD-5597 is a potent CDK inhibitor with IC50 values of 2 nM for CDK1 and CDK2, respectively [1]. The cyclin-dependent kinases (CDKs) are serine-threonine protein kinases with roles in the regulation of the cell cycle, and also involved in regulating transcription, mRNA processing, and the differentiation of nerve cells [1]. AZD-5597 is a potent imidazole pyrimidine amide CDK inhibitor. In LoVo cells, AZD-5597 exhibited high level of anti-proliferative activity with IC50 value of 0.039 μM. AZD-5597 exhibited excellent aqueous solubility ( > 50 mg/mL), photostability (t1/2 > 24 h), hydrolytic stability (pH 4-10, t1/2 > 100 days), plasma stability ( > 18 h) and the lack of CYP inhibition. The overall profile of AZD-5597 indicated that it was suitable for further development as an iv agent [1]. In nude mouse and rat, AZD-5597 possessed good pharmacokinetic parameters with moderate to low clearance. In nude mice implanted subcutaneously with SW620 human colon adenocarcinoma cells, AZD-5597 (15 mg/kg, dosed intermittently for 3 weeks, ip) inhibited tumour volume by 55% [1].
- Properties
  - Alternative Name
    
    (S)-(4-((5-fluoro-4-(1-isopropyl-2-methyl-1H-imidazol-5-yl)pyrimidin-2-yl)amino)phenyl)(3-(methylamino)pyrrolidin-1-yl)methanone
    
    CAS Number
    
    924641-59-8
    
    Molecular Formula
    
    C23H28FN7O
    
    Molecular Weight
    
    437.51
    
    Appearance
    
    A solid
    
    Purity
    
    99.54%
    
    Solubility
    
    ≥1.82 mg/mL in H2O with ultrasonic; ≥12.7 mg/mL in EtOH; ≥15.65 mg/mL in DMSO
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only

AZD-5597

Background

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