| 靶点: |
IC50: 0.22 µM (Abl) |
| 体内研究: |
GNF-5 (5 mg/kg iv. or 20 mg/kg oral) has suitable pharmacokinetic parameters. GNF-5 (oral, 50 or 100 mg/kg, twice daily, for 7 days) shows efficacious in vivo but can observe relapses. GNF-5 (75 mg/kg, b.i.d) inhibits T315I Bcr-Abl combination with nilotinib in vivo. |
| 参考文献: |
1. Zhang J, et al. Targeting Bcr-Abl by combining allosteric with ATP-binding-site inhibitors. Nature. 2010 Jan 28;463(7280):501-6. 2. Meirson T, et al. Targeting invadopodia-mediated breast cancer metastasis by using ABL kinase inhibitors. Oncotarget. 2018 Apr 24;9(31):22158-22183. |
| 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 |
2.39 ml |
11.951 ml |
23.902 ml |
| 5 mM |
0.478 ml |
2.39 ml |
4.78 ml |
| 10 mM |
0.239 ml |
1.195 ml |
2.39 ml |
| 50 mM |
0.048 ml |
0.239 ml |
0.478 ml |
|
| 注意: |
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