Flavopiridol

- Overview
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    Background
    
    Flavopiridol is a potent and selective inhibitor of cyclin-dependent kinases (CDKs) with IC50 values of ~41 nM for CDK1, CDK2, CDK4, CDK6 and 300 nM for CDK7, respectively [1].CDKs are a family of protein kinases regulating the cell cycle and play an important role in transcription, mRNA processing, and cell differentiation.Analysis of the crystal structure suggested flavopiridol binded to the ATP-binding pocket of CDK2. In MCF-7 breast cancer cells, flavopiridol reduced the mRNA level of cyclin D1 protein and cyclin D3 protein [1]. In 23 human tumor cell models, flavopiridol significantly inhibited human bone marrow colony formation between 10 and 100 ng/ml [2].In prostate cancer xenograft PRXFI369, flavopinidol (10 mg/kg/day) had antitumor activity of optimal test/control (T/C) of 33% and a growth delay of 30 days. Also, it reduced tumor volume by 85%. In prostate cancer xenograft PRXFI337, the optimal T/C was 27% and the growth delay was 17 days [2].
    
    [1]. Senderowicz AM. The cell cycle as a target for cancer therapy: basic and clinical findings with the small molecule inhibitors flavopiridol and UCN-01. Oncologist, 2002, 7 Suppl 3: 12-9.
    [2]. Drees M, Dengler WA, Roth T, et al. Flavopiridol (L86-8275): selective antitumor activity in vitro and activity in vivo for prostate carcinoma cells. Clin Cancer Res, 1997, 3(2): 273-279.
    [3]. Carlson BA, Dubay MM, Sausville EA, et al. Flavopiridol induces G1 arrest with inhibition of cyclin-dependent kinase (CDK) 2 and CDK4 in human breast carcinoma cells. Cancer Res, 1996, 56(13): 2973-2978.
- Properties
  - Alternative Name
    
    L868275; HMR-1275; Alvocidib; 2-(2-chlorophenyl)-5,7-dihydroxy-8-[(3S,4R)-3-hydroxy-1-methylpiperidin-4-yl]chromen-4-one
    
    CAS Number
    
    146426-40-6
    
    Molecular Formula
    
    C21H20ClNO5
    
    Molecular Weight
    
    401.85
    
    Appearance
    
    A crystalline solid
    
    Purity
    
    Purity ≥ 95.00%
    
    Solubility
    
    insoluble in H2O; ≥40.2 mg/mL in DMSO; ≥85.4 mg/mL in EtOH with gentle warming and ultrasonic
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only

Flavopiridol

Background

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