产品描述: | CNX-774 is an orally active, irreversible and selective BTK inhibitor, with an IC50 of < 1 nM. CNX-774 specifically targets Cysteine 481 of Btk for covalent modification |
靶点: |
IC50: 1 nM (BTK);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. |
溶解性: |
DMSO : ≥ 45 mg/mL (90.09 mM) |
保存条件: |
2-8℃ |
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。 |