CNX-500

Names

[ CAS No. ]:
1202758-21-1

[ Name ]:
CNX-500

Biological Activity

[Description]:

CNX-500 is a probe consisting of a covalent Btk inhibitor (CC-292) chemically linked to biotin. CNX-500 retains inhibitory activity against Btk (IC50 of 0.5 nM) and the ability to form a covalent bond with Btk. CNX-500 has low inhibitory effects on kinase epidermal growth factor receptor, and upstream Src-family kinases including Syk and Lyn[1].

[Related Catalog]:

Research Areas >> Cancer

Signaling Pathways >> Protein Tyrosine Kinase/RTK >> Btk

[In Vitro]

Used in a competition assay, CNX-500 detects free, uninhibited Btk and is excluded from interaction with Btk previously bonded by CC-292. In Ramos cells exposed to a range of CC-292 concentrations, the amount of Btk captured by the probe is compared with untreated samples and the extent of Btk bonded is demonstrated to be proportional to CC-292 drug concentration[1].

[References]

[1]. Evans EK, et al. Inhibition of Btk with CC-292 provides early pharmacodynamic assessment of activity in mice and humans. J Pharmacol Exp Ther. 2013 Aug;346(2):219-28.

Chemical & Physical Properties

[ Molecular Formula ]:
C₄₈H₆₈N₁₀O₉S

[ Molecular Weight ]:
961.18

CNX-500

Names

Biological Activity

Chemical & Physical Properties

Related Compounds