1202759-32-7

Basic information

• Product Name: CNX-774
• Synonyms: CNX-774;4-[4-[[5-Fluoro-4-[[3-[(1-oxo-2-propen-1-yl)amino]phenyl]amino]-2-pyrimidinyl]amino]phenoxy]-N-methyl-2-pyridinecarboxamide;4-(4-((4-((3-acrylamidophenyl)amino)-5-fluoropyrimidin-2-yl)amino)phenoxy)-N-methylpicolinamide;4-[4-[[5-Fluoro-4-[[3-[(1-oxo-2-propen-1-yl)amino]phenyl]amino]-2-pyrimidinyl]amino]phenoxy]-N-methyl-2-pyridinecarboxamide CNX-774;4-(4-((4-((3-Acrylamidophenyl)amino)-5-fluoropyrimidin-2-yl)amino)phenoxy)-N-methylpicolinamid;2-Pyridinecarboxamide, 4-[4-[[5-fluoro-4-[[3-[(1-oxo-2-propen-1-yl)amino]phenyl]amino]-2-pyrimidinyl]amino]phenoxy]-N-methyl-
• CAS NO: 1202759-32-7
• Molecular Formula: C26H22FN7O3
• Molecular Weight: 499.4963832
• Product Categories: Inhibitors
• Mol File: 1202759-32-7.mol
• Article Data: 1

Chemical Properties

• Appearance: /
• Density: 1.383±0.06 g/cm3(Predicted)
• Solubility: Soluble in DMSO
• PKA: 13.22±0.70(Predicted)
• CAS DataBase Reference: CNX-774(CAS DataBase Reference)
• NIST Chemistry Reference: CNX-774(1202759-32-7)
• EPA Substance Registry System: CNX-774(1202759-32-7)

Safety Data

• Hazardous Substances Data: 1202759-32-7(Hazardous Substances Data)

Usage

Description

CNX-774 is an innovative pharmaceutical compound that functions as an irreversible, orally active, and highly selective inhibitor of Bruton's tyrosine kinase (BTK). This characteristic positions it as a promising therapeutic agent for various medical applications, particularly in the management of inflammatory and autoimmune conditions.

Uses

Used in Pharmaceutical Industry:
CNX-774 is used as an anti-inflammatory agent for its ability to modulate the immune response and alleviate symptoms associated with inflammatory diseases.
Used in Autoimmune Disease Treatment:
CNX-774 is used as a therapeutic intervention for rheumatoid arthritis (RA) due to its capacity to target and inhibit the BTK enzyme, which plays a crucial role in the pathogenesis of RA. By doing so, CNX-774 helps in reducing inflammation and joint damage, thereby improving the quality of life for patients suffering from this debilitating condition.
Furthermore, given its selectivity and mechanism of action, CNX-774 may also hold potential for the treatment of other autoimmune and inflammatory disorders, although these applications would require additional research and clinical validation.

Biological Activity

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].

references

[1]. akinleye a, chen y, mukhi n, et al. ibrutinib and novel btk inhibitors in clinical development. j hematol oncol, 2013, 6: 59.

Relevant articles and documents

HETEROARYL COMPOUNDS AND USES THEREOF

The present invention provides inhibitors of protein kinases of formula I-a and I-b, pharmaceutically acceptable compositions thereof, and methods of using the same.