| 货号 | 12209S |
| 供应商 | CST |
| 背景 | Nilotinib (AMN-107) is a novel tyrosine kinase inhibitor that potently inhibits Bcr-Abl. Nilotinib is more effective than imatinib at decreasing the proliferation and viability in cells expressing wild-type Bcr-Abl and is active against many imatinib-resistant Bcr-Abl mutants, with the exception of T315I (1-4). Nilotinib has been shown to inhibit Abl activity in cells expressing wild-type Abl and imatinib-resistant mutant Abl, with ~20-fold greater potency than imatinib. Nilotinib is similarly effective at inhibiting Abl autophosphorylation (3). Research studies have demonstrated that nilotinib treatment of Bcr-Abl-expressing K-562 cells attenuates Stat5 and CrkL phosphorylation, decreases Bcl-xL and c-Myc expression, induces p27 and Bim expression, and induces PARP cleavage. Many of these effects are enhanced by cotreatment with the histone deacetylase inhibitor LBH589 (5). |
| 存放说明 | -20C |
| 参考文献 | 1 . Weisberg, E. et al. (2006) Br J Cancer 94, 1765-9. 2 . Golemovic, M. et al. (2005) Clin Cancer Res 11, 4941-7. 3 . OHare, T. et al. (2005) Cancer Res 65, 4500-5. 4 . Weisberg, E. et al. (2005) Cancer Cell 7, 129-41. 5 . Fiskus, W. et al. (2006) Blood 108, 645-52. |
Chemical structure of nilotinib.尼罗替尼的化学结构。 | |
Western blot analysis of extracts from K-562 cells, untreated (-) or treated (+) with Nilotinib (1000 nM, 24 hr), using PathScan® Bcr/Abl Activity Assay: Phospho-c-Abl, Phospho-Stat5, and Phospho-CrkL Multiplex Western Detection Cocktail #5300 to detect inhibition of phospho-Bcr-Abl, phospho-Stat5, and phospho-CrkL.Western blot方法检测K-562细胞提取物，细胞不处理（-）或用尼罗替尼(1000 nM, 24 hr)处理（+），使用PathScan Bcr/ Abl活性分析：磷酸化c-Abl，磷酸化Stat5和磷酸化CrkL的多重Western检测混合物＃5300，以检测对磷酸化Bcr-Abl，磷酸化Stat5，磷酸化CrkL的抑制。 |
