179324-69-7

溶解度:Soluble in DMSO at 200mg/mL, ethanol at 200mg/mL

储存条件:-20C 2 years

生物活性

Bortezomib blocks TNF-induced NF-kB activation in a dose- and time-dependent fashion in multiplemyeloma cells through degradation of IkB. Bortezomib caused comparable growth suppression in LNCaP-Pro5 and PC3M-Pro4 cells with an IC90 of 10 nM. Bortezomib inhibits cell proliferation of H460 cells (Human non-small cell lung cancer cell lines) with an IC50 of 0.1 µM. In a study with the National Cancer Institute's panel of 60 human cell lines, bortezomib showed a mean IC50 of 7 nM as tested by SRB analysis.

参考文献

1. The proteasome: a suitable antineoplastic target. Adams,Julian; Nature Reviews Cancer; 1474-175X; 20040500; 4(5);349-360 2. Fresh from the pipeline: Bortezomib Paramore,Andrew; Frantz,Simon; Nature Reviews Drug Discovery; 1474-1776; 20030800 ; 2(8); 611-612; 10.1038/nrd1159 3. Adams, J., et al. "Proteasome inhibitors: a novel class of potent and effective antitumor agents." Cancer Res. 59: 2615-2622 (1999). 4. Williams, S., et al. "Differential effects of the proteasome inhibitor bortezomib on apoptosis and angiogenesis in human prostate tumor xenografts." Mol. Cancer Ther. 2: 835-843 (2003). 5. Ling, Y., et al. "Mechanisms of Proteasome Inhibitor PS-341-induced G2-M-Phase Arrest and Apoptosis in Human Non-Small Cell Lung Cancer Cell Lines." Clin. Cancer Res. 9: 1145-1154 (2003).