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    CNX-774
    CNX-774

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V0645
    CAS #: 1202759-32-7Purity ≥98%

    Description: CNX-774 (CNX774) is an irreversible/covalent, orally bioavailable, and highly selective inhibitor of BTK (Bruton's tyrosine kinase) with potential anticancer activity. It inhibits BTK with an IC50 of<1 nM. CNX-774 acts by forming a covalent bond with the Cys-481 residue within the active site of BTK, which is an key enzyme in the B-cell antigen receptor (BCR) signaling pathway, and also plays an pivotal role in the maturation of mast cells activation and B cells. 

    References: 17th North Am Meet Int Soc Study Xenobiot.

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    Molecular Weight (MW)499.5
    FormulaC26H22FN7O3
    CAS No.1202759-32-7
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 100 mg/mL (200.2 mM)
    Water: <1 mg/mL
    Ethanol: 2 mg/mL (4.0 mM)
    SMILESO=C(NC)C1=NC=CC(OC2=CC=C(NC3=NC=C(F)C(NC4=CC=CC(NC(C=C)=O)=C4)=N3)C=C2)=C1 
    SynonymsCNX 774; CNX-774; CNX774;  

    Chemical Name: 4-(4-((4-((3-acrylamidophenyl)amino)-5-fluoropyrimidin-2-yl)amino)phenoxy)-N-methylpicolinamide

    InChi Key: VVLHQJDAUIPZFH-UHFFFAOYSA-N

    InChi Code: InChI=1S/C26H22FN7O3/c1-3-23(35)31-17-5-4-6-18(13-17)32-24-21(27)15-30-26(34-24)33-16-7-9-19(10-8-16)37-20-11-12-29-22(14-20)25(36)28-2/h3-15H,1H2,2H3,(H,28,36)(H,31,35)(H2,30,32,33,34)


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    In Vitro

    In vitro activity: CNX-774 is a potent, irreversible/covalent, orally bioactive, and highly selective BTK (Bruton’s tyrosine kinase) inhibitor with IC50 of<1 nM. It forms a ligand-directed covalent bond with Cys-481, a non-conserved amino acid within the active site of the enzyme.


    Kinase Assay: 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. 


    Cell Assay:  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. 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.

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    References J Hematol Oncol. 2013 Aug 19;6:59.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

    CNX-774

    BTK structure. BTK belongs to the Tec family of protein tyrosine kinases and is composed of the PH (pleckstrin homology), TH (Tec homology), SH3 (Src homology 3) SH2 (Src homology 2), and SH 1/TK (Src homology1/Tyrosine kinase) domains. Binding sites for BTK substrates, inhibitors, and upstream molecules are shown in the diagram.  2013 Aug 19;6:59.

    CNX-774



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