化学名称 : 4-[2-甲基-1-异丙基-1H-咪唑-5-基]-N-[4-(甲磺酰基)苯基]-2-嘧啶胺
CAS : 602306-29-6
英文名称: AZD 5438/AZD-5438
英文同义词: 4-[2-Methyl-1-(1-methylethyl)-1H-im idazol-5-yl]-N-[4-(methylsulfonyl)phenyl]-2-pyrimi dinamine
同义词: 4-[2-甲基-1-异丙基-1H-咪唑-5-基]-N-[4-(甲磺酰基)苯基]-2-嘧啶胺
溶解度:DMSO
储存条件:-20℃ 2 years
生物活性
Nanomolar concentrations of flavopiridol inhibited rhabdoid cell growth (IC50-200nmol/L) , induced G1and G2 arrest, and apoptosis in vitro in a concentration-dependent manner. These effects were correlated with the down-modulation of cyclin D1, up-regulation of p21, and induction of caspase 3/7 activities. Flavopiridol (at 7.5 mg/kg) significantly inhibited the growth of xenografted rhabdoid tumors, and its effect was correlated with the induction of p21 and down-modulation of cyclin D1. [2]
Exposure of HNSCC cells to flavopiridol diminished cdc2 and cdk2 activity and potently inhibited cell proliferation (IC50=43-83 nM), which was concomitant with the appearance of cells with a sub-G1 DNA content. [3]
参考文献
[1] Lloyd R Kelland . Expert Opinion on Investigational Drugs. 2000 December;9(12):2903-2911
[2] Melissa E. Smith et al. Clin Cancer Res.2008 January 15;14:523-532
[3] Vyomesh Patel et al. The Journal of Clinical Investigation. 1998 November;102(9):1674-1681