| 体内研究: |
GZD856 (10-30 mg/kg, p.o. once daily for 16 d) displays good antitumor activity in both H1703 and A549 lung cancer models and is well tolerated. GZD856 inhibits brain and liver metastasis of lung cancer cells in an A549-Luc orthotopic model. GZD856 (10 mg/kg; p.o. once daily for 8 d) potently inhibits tumor growth in mouse bearing xenograft K562 and Ba/F3 cells expressing Bcr-AblT315I. GZD856 (5 mg/kg; a single i.v.) exhibits a long half-life (T1/2=19.97 h), optimal plasma exposure (Cmax=934.38 μg/L) and a AUC0-∞ (8165.8 μg/L h) in rats. GZD856 (25 mg/kg; a single p.o.) exhibits a long half-life (T1/2=22.2 h), optimal plasma exposure (Cmax=899.5 μg/L) and a good oral bioavailability (BA=78%) in rats. |
| 参考文献: |
1. Zhang Z, et, al. GZD856, a novel potent PDGFRα/β inhibitor, suppresses the growth and migration of lung cancer cells in vitro and in vivo. Cancer Lett. 2016 May 28;375(1):172-178. 2. Lu X, et, al. Synthesis and identification of GZD856 as an orally bioavailable Bcr-Abl T315I inhibitor overcoming acquired imatinib resistance. J Enzyme Inhib Med Chem. 2017 Dec;32(1):331-336. |
| 保存条件: |
-80℃,干燥(运输条件:冰袋低温运输) |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
1.728 ml |
8.642 ml |
17.284 ml |
| 5 mM |
0.346 ml |
1.728 ml |
3.457 ml |
| 10 mM |
0.173 ml |
0.864 ml |
1.728 ml |
| 50 mM |
0.035 ml |
0.173 ml |
0.346 ml |
|
| 注意: |
部分产品我司仅能提供部分信息,我司不保证所提供信息的权威性,仅供客户参考交流研究之用。 |