Flavopiridol (Synonyms: Alvocidib, HL 275, HMR 1275, L-868,275) |
Catalog No.GC16063 |
An inhibitor of cyclin-dependent kinases
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Cas No.: 146426-40-6
Sample solution is provided at 25 µL, 10mM.
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].
References:
[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.
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