| 产品描述: | SHR2415 is a highly potent, selective and orally active ERK1/2 inhibitor. SHR2415 has inhibition activity for ERK1 and ERK2 with IC50 values of 2.8 nM and 5.9 nM, respectively. SHR2415 exhibits high potency with an IC50 value of 44.6 nM in Colo205 cells. SHR2415 can be used for the research of cancer. |
| 靶点: |
ERK1:2.8 nM (IC50); ERK2:5.9 nM (IC50) |
| 体外研究: |
SHR2415 (i.v. (1 mg/kg for mouse and rat) and p.o. (2 mg/kg for mouse, rat, and dog)) displays a favorable PK profile across species with low clearance and good in vivo exposure. SHR2415 (25, 50 mg/kg; p.o.; once daily, for 14 days) displays favorable PK profiles across species as well as robust in vivo efficacy in a mouse Colo205 xenograft model. |
| 体内研究: |
SHR2415 has inhibition activity for ERK1 and ERK2 with IC50 values of 2.8 nM and 5.9 nM, respectively. SHR2415 shows the cellular potency with an IC50 value of 44.6 nM in Colo205 cells. |
| 参考文献: |
1. Xin Li, et al. Discovery of SHR2415, a Novel Pyrrole-Fused Urea Scaffold ERK1/2 Inhibitor. ACS Med Chem Lett. 2022 Apr 1;13(4):701-706. |
| 保存条件: |
-20°C |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
2.156 ml |
10.778 ml |
21.555 ml |
| 5 mM |
0.431 ml |
2.156 ml |
4.311 ml |
| 10 mM |
0.216 ml |
1.078 ml |
2.156 ml |
| 50 mM |
0.043 ml |
0.216 ml |
0.431 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。 |