CNX-774 |
| カタログ番号GC13439 |
CNX-774 は、IC50 が 1 nM 未満の、経口で活性な、不可逆的かつ選択的な BTK 阻害剤です。 CNX-774 は、共有結合修飾のために Btk のシステイン 481 を特異的に標的とします。
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Cas No.: 1202759-32-7
Sample solution is provided at 25 µL, 10mM.
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CNX-774 is an orally active and selective inhibitor of BTK with IC50 value of <1 nM.
Bruton’s tyrosine kinase (BTK) is an important enzyme in the B-cell antigen receptor (BCR) signaling pathway and also plays an important role in mast cell activation and B cell maturation.
CNX-774 is an orally active, irreversible and selective BTK inhibitor with IC50 value of <1 nM. CNX-774 formed covalent bond with the Cys481 residue within the ATP binding site of BTK. In cellular assays, CNX-774 inhibited BTK with IC50 values of 1-10 nM [1].
Reference:
[1]. Akinleye A, Chen Y, Mukhi N, et al. Ibrutinib and novel BTK inhibitors in clinical development. J Hematol Oncol, 2013, 6: 59.
Average Rating: 5 (Based on Reviews and 7 reference(s) in Google Scholar.)
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