货号 | 8705S |
供应商 | CST |
背景 | Sorafenib, also known as Bay 43-9006, is a novel multikinase inhibitor that targets the RAF family of serine/threonine kinases and tyrosine kinase receptors involved in tumor progression and tumor angiogenesis, including: VEGFR-2 (IC50 = 90 nM), VEGFR-3 (IC50 = 20 nM), PDGFR- (IC50 = 57 nM), c-KIT (IC50 = 68 nM), and Flt3 (IC50 = 58 nM) (1). Research studies have demonstrated that sorafenib induces apoptosis in several tumor cell lines through the down-regulation of the antiapoptotic protein myeloid cell leukemia-1 (Mcl-1). Down-regulation of Mcl-1 by sorafenib is associated with the release of cytochrome c from mitochondria into the cytosol and caspase activation, leading to apoptotic cell death (2). STAT3 inhibition by sorafenib has been observed in multiple cell types (3-5). |
存放说明 | -20C |
参考文献 | 1 . Wilhelm, S.M. et al. (2004) Cancer Res 64, 7099-109. 2 . Yu, C. et al. (2005) Oncogene 24, 6861-9. 3 . Zhao, W. et al. (2011) Anticancer Drugs 22, 79-88. 4 . Huang, S. and Sinicrope, F.A. (2010) Mol Cancer Ther 9, 742-50. 5 . Yang, F. et al. (2008) Mol Cancer Ther 7, 3519-26. |
Chemical structure of sorafenib.索拉菲尼的化学结构。 | |
Western blot analysis of extracts from NIH/3T3 cells, serum-starved overnight and untreated or treated with hPDGF-BB #8912 (100 ng/ml, 5 min) either with or without sorafenib pre-treatment (1 µM, 2 hr), using Phospho-PDGF Receptor β (Tyr1009) (42F9) Rabbit mAb #3124 (upper) or PDGF Receptor β (28E1) Rabbit mAb #3169 (lower).Western blot方法检测NIH/3T3细胞提取物,细胞经血清饥饿过夜后,不处理或用hPDGF-BB #8912 (100 ng/ml, 5 min)处理,用或不用索拉菲尼进行预处理(1 µM, 2 hr),使用的抗体为Phospho-PDGF Receptor β (Tyr1009) (42F9) Rabbit mAb #3124 (上图)或PDGF Receptor β (28E1) Rabbit mAb #3169 (下图). |