Cas No.: | 1202758-21-1 |
Chemical Name: | CNX-500 |
Synonyms: | CNX500,CNX 500 |
SMILES: | CC(C=N1)=C(NC2=CC(NC(C=C)=O)=CC=C2)N=C1NC3=CC=CC(OCCCNC(CCCC(NCCCOCCOCCOCCCNC(CCCC[C@H]4[C@@H](NC5=O)[C@@H](N5)CS4)=O)=O)=O)=C3 |
Formula: | C48H68N10O9S |
M.Wt: | 961.18 |
Purity: | >99% |
Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
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]. |
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. |