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  • CNX-774

    货号: abs818594
    CAS号: 1202759-32-7
    分子式: C26H22FN7O3
    分子量: 499.5
    产品说明书
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    货号-规格 货期 价格 数量
    abs818594-2mg 1-2周 ¥931.00
    - +
    abs818594-5mg 1-2周 ¥1415.00
    - +
    abs818594-10mg 1-2周 ¥2496.00
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    大包装询价
    产品描述
    描述

     CNX-774 is a potent, selective, and orally available small molecule inhibitor of Btk (IC50< 1 nM) that forms a ligand-directed covalent bond with Cys-481, a non-conserved amino acid within the active site of the enzyme. IC50 Value: <1 nM Target: Btk Kinase In biochemical assays, CNX-774 has demonstrated potent inhibition of Btk with an IC50 of <1nM in a continuous-read assay. The covalent bonding of CNX-774 to Btk was confirmed by incubating recombinant Btk protein with a 10-fold molar excess of CNX-774 for 1 hour at room temperature and analysis by MALDI-TOF MS. A shift of protein mass corresponding to the molecular weight of CNX-774 confirmed the covalent bonding of CNX-774 to Btk. Digestion of the covalently bonded Btk with pepsin followed by MSMS analysis established the bonding of CNX-774 to Cys-481. Cellular potency as well as prolonged duration of action of CNX-774 was demonstrated in Ramos cells by using a biotinylated covalent probe that targets the same Cysteine residue as CNX-774. CNX-774 was found to be >90% extractable after 2 hrs of incubation in both rat and human whole blood. These results demonstrate that CNX-774 has 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.

    纯度
    ≥98%
    储存/保存方法
    Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.
    基本信息
    可溶性/溶解性
    Ethanol:2mg/mL(4.0mM)
    DMSO:100mg/ml(200.2 mM)
    生物活性
    靶点
    BTK
    In vitro(体外研究)
    In cellular assays, CNX-774 demonstrates potent inhibitory activity towards BTK with IC50 of 1-10 nM by targeting Cys-481 residue within the ATP binding site of the enzyme.
    参考文献
    参考文献
    温馨提示:本产品仅作科研实验使用,不支持临床等研究
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