| 产品描述: | Zefamenib (BN-104) is an effective selective brain membrane protein inhibitor with oral activity, and it's also a Menin inhibitor, it can block the Menin-MLL interaction and leads to the degradation of Menin protein. Zefamenib is a weak hERG inhibitor, with an IC50 greater than 100 μM. Zefamenib has anti-tumor activity and can be used in cancer research, such as for acute myeloid leukemia. |
| 靶点: |
hERG:>100 μM (IC50) |
| 体外研究: |
Zefamenib (BN-104) (0-60 mg/kg,口服,一天两次,21 天) 在小鼠模型中抑制肿瘤增殖。 |
| 体内研究: |
Zefamenib (BN-104) 抑制白血病细胞增殖, IC50 值分别为: MV-4-11 AF4 fusion (3.5 nM); MOLM13 AF9 fusion(12 nM); OCI-AML3 NPM1 mutant (11 nM)。 Zefamenib (10 μM,0-24 h) 在 MV-4-11 细胞中导致 Menin 蛋白降解。 |
| 参考文献: |
1. Taishan Hu, et al. "Discovery of a novel menin-MLL inhibitor for potential treatment of MLLr leukemias and NPM1c AML." Cancer Research. Vol. 82. No. 12. 615 CHESTNUT ST, 17TH FLOOR, PHILADELPHIA, PA 19106-4404 USA: AMER ASSOC CANCER RESEARCH, 2022. |
| 保存条件: |
-80°C 6个月;-20°C 1个月 |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
1.752 ml |
8.762 ml |
17.524 ml |
| 5 mM |
0.35 ml |
1.752 ml |
3.505 ml |
| 10 mM |
0.175 ml |
0.876 ml |
1.752 ml |
| 50 mM |
0.035 ml |
0.175 ml |
0.35 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。 |