745833-23-2

Basic information

• Product Name: VX 702
• Synonyms: 6-[(Aminocarbonyl)(2,6-difluorophenyl)amino]-2-(2,4-difluorophenyl)-3-pyridinecarboxamide;VX 702;6-[(Aminocarbonyl)(2,6-difluorophenyl)amino]-2-(2,4-difluorophenyl)-3-pyridinecarboxamide VX-702;VX 702 6-[(Aminocarbonyl)(2,6-difluorophenyl)amino]-2-(2,4-difluorophenyl)-3-pyridinecarboxamide;2-(2,4-Difluorophenyl)-6-(1-(2,6-difluorophenyl)ureido)nicotinamide
• CAS NO: 745833-23-2
• Molecular Formula: C₁₉H₁₂F₄N₄O₂
• Molecular Weight: 404.3177928
• Product Categories: Aromatics;Heterocycles;Intermediates & Fine Chemicals;Pharmaceuticals;Protein Kinase Inhibitors and Activators;Inhibitors
• Mol File: 745833-23-2.mol
• Article Data: 2

Chemical Properties

• Boiling Point: 555.2±60.0 °C(Predicted)
• Appearance: /
• Density: 1.503
• Storage Temp.: -20°C
• Solubility: Soluble in DMSO (up to 40 mg/ml) or in Ethanol (up to 2 mg/ml)
• PKA: 10.65±0.50(Predicted)
• Stability: Stable for 2 years from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 3 months.
• CAS DataBase Reference: VX 702(CAS DataBase Reference)
• NIST Chemistry Reference: VX 702(745833-23-2)
• EPA Substance Registry System: VX 702(745833-23-2)

Safety Data

• Hazardous Substances Data: 745833-23-2(Hazardous Substances Data)

Usage

Description

VX 702 is a third-generation inhibitor of p38 mitogen-activated protein (MAP) kinases, which binds to both p38α and p38β in an ATP-competitive manner. It is known for its ability to inhibit the production of IL-6, IL-1β, and TNF-α in LPS-primed blood and suppress the activation of p38 in platelets by various stimuli. However, it does not block platelet aggregation in response to collagen and provides only transient suppression of biomarkers of inflammation in ongoing rheumatoid arthritis.

Uses

Used in Pharmaceutical Industry:
VX 702 is used as an anti-inflammatory agent for its potential in treating inflammation, rheumatoid arthritis, and cardiovascular diseases. Its ability to inhibit p38 MAP kinases and reduce the production of inflammatory cytokines makes it a promising candidate for these applications.
Used in Research Applications:
VX 702 is used as a research tool for studying the role of p38 MAP kinases in various cellular processes and diseases. Its selective inhibition of p38α and p38β allows researchers to investigate the specific functions and pathways associated with these kinases, contributing to a better understanding of their biological significance.

Biological activity

VX-702 is a highly selective p38α MAPK inhibitor, 14-fold more potent against p38α than against p38β. Phase 2.

References

1) Goldstein?et al.?(2010),?Selective p38alpha inhibitors clinically evaluated for the treatment of chronic inflammatory disorders; J. Med. Chem.,?53?2345 2) Kuliopulos?et al.?(2004),?Effect of selective inhibition of the p38 MAP kinase pathway on platelet aggregation; Thromb. Haemostasis,?92?1387 3) Damianov?et al.?(2009),?Efficacy, pharmacodynamics, and safety of VX-702, a novel p38 MAPK inhibitor, in rheumatoid arthritis: results of two randomized, double-blind, placebo-controlled clinical studies; Arthrit. Rheumat.,?60?1232 4) Ding?et al. (2006),?Drug evaluation: VX-702, a MAP kinase inhibitor for rheumatoid arthritis and acute coronary syndrome; Curr. Opin. Investig. Drugs,?7?1020 5) Scripchenko?et al.?(2013),?An inhibition of p38 mitogen activated protein kinase delays the platelet storage lesion; PLoS One,?8(8)e?70732

Upstream product

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Relevant articles and documents

SOLID FORMS OF 2-(2, 4-DIFLUOROPHENYL)-6-(1-(2,6-DIFLUOROPHENYL)UREIDO)NICOTINAMIDE

This invention relates to solid forms of 2-(2, 4-difluorophenyl)-6-(l- (2,6-difluorophenyl)ureido)nicotinamide and pharmaceutical compositions thereof, and methods and uses therewith.