CNX-500
Cat. No.: DC28073
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Chemical Structure
1202758-21-1
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Field of application
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.
| 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. |
MSDS
| TITLE |
DOWNLOAD |
| MSDS_12129_DC28073_1202758-21-1 |
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| LOT NO. |
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