| 靶点: |
Ki: 7.5 nM (Syk);IC50: 10 nM (Syk) |
| 体内研究: |
Bay 61-3606 (50 mg/kg;通过腹膜内注射每周给药两次,持续两周) 导致比单独使用 TNF 相关凋亡诱导配体 (TRAIL;10 mg/kg) 更有效地减少 BALB/c 裸鼠的 MCF-7异种移植肿瘤。Bay 61-3606 与 TRAIL 组合给药可显著减小异种移植肿瘤的体积。 |
| 参考文献: |
1. Yamamoto N, et al. The orally available spleen tyrosine kinase inhibitor 2-[7-(3,4-dimethoxyphenyl)-imidazo[1,2-c]pyrimidin-5-ylamino]nicotinamide dihydrochloride (BAY 61-3606) blocks antigen-induced airway inflammation in rodents. J Pharmacol Exp Ther. 2003 Sep;306(3):1174-81. 2. Tümmler C, et al. SYK Inhibition Potentiates the Effect of Chemotherapeutic Drugs on Neuroblastoma Cells in Vitro. Cancers (Basel). 2019 Feb 10;11(2). pii: E202. 3. Gioia R, et al. Quantitative phosphoproteomics revealed interplay between Syk and Lyn in the resistance to AMN107 in chronic myeloid leukemia cells. Blood. 2011 Aug 25;118(8):2211-21. 4. Kim SY, et al. Bay 61-3606 Sensitizes TRAIL-Induced Apoptosis by Downregulating Mcl-1 in Breast Cancer Cells. PLoS One. 2015 Dec 31;10(12):e0146073. |
| 保存条件: |
-80℃(运输条件:冰袋低温运输) |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
2.158 ml |
10.792 ml |
21.583 ml |
| 5 mM |
0.432 ml |
2.158 ml |
4.317 ml |
| 10 mM |
0.216 ml |
1.079 ml |
2.158 ml |
| 50 mM |
0.043 ml |
0.216 ml |
0.432 ml |
|
| 注意: |
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