| 产品描述: | BTK抑制剂;BTK Inhibitors;;InformationCNX-774 CNX-774 is an irreversible, orally active, and highly selective BTK inhibitor with IC50 of <1 nM.TargetsBTK <1 nMIn vitroIn cellular assays, CNX-774 demonstrates potent inhibitory activity towards BTK with IC50 of 1-10 nM by targeting Cys-481 residue within the ATP binding site of the enzyme. |
| 靶点: |
IC50: 1 nM (BTK). |
| 体内研究: |
CNX-774 is stable and non-reactive in fresh human and rat whole blood and does not covalently bond to any of the mid-level abundance human plasma proteins. CNX-774 demonstrates potent inhibitory activity towards the intended target, Btk, while achieving remarkable specificity in a variety of assays designed to assess off-target reactivity towards abundant cellular thiols and blood proteins. |
| 参考文献: |
1. Matthew Labenski, et al. In Vitro Reactivity Assessment of Covalent Drugs Targeting Bruton's Tyrosine Kinase.2. Akintunde Akinleye, et al. Ibrutinib and novel BTK inhibitors in clinical development. J Hematol Oncol. 2013 Aug 19;6:59. |
| 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 |
2.002 ml |
10.01 ml |
20.02 ml |
| 5 mM |
0.4 ml |
2.002 ml |
4.004 ml |
| 10 mM |
0.2 ml |
1.001 ml |
2.002 ml |
| 50 mM |
0.04 ml |
0.2 ml |
0.4 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。 |