VX 702 Property

Boiling point:

555.2±60.0 °C(Predicted)

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)

form 

solid

color 

White

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

745833-23-2

Safety

HS Code 

2933399990

Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H315Causes skin irritation

H319Causes serious eye irritation

Precautionary statements

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P302+P352IF ON SKIN: wash with plenty of soap and water.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

P332+P313IF SKIN irritation occurs: Get medical advice/attention.

P337+P313IF eye irritation persists: Get medical advice/attention.

VX 702 Chemical Properties,Usage,Production

Biological activity

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

Description

VX-702 is a third generation inhibitor of p38 mitogen-activated protein (MAP) kinases, binding to both p38α and p38β (K_d = 3.7 and 17 nM, respectively) in an ATP-competitive fashion. It inhibits IL-6, IL-1β, and TNF-α production in LPS-primed blood with IC₅₀ values of 59, 122, and 99 ng/ml, respectively. VX-702, at 1 μM, inhibits activation of p38 in platelets by thrombin, U-46619 , or collagen but does not block platelet aggregation in response to collagen. Although orally active, VX-702 provides only transient suppression of biomarkers of inflammation in ongoing rheumatoid arthritis.

Uses

VX-702 is a p38 mitogen-activated protein kinase (MAPK) inhibitor. VX-702 had no effect on platelet aggregation induced by any of the p38 MAPK agonists. VX-702 has potential use in the treatment of inflammation, rheumatoid arthritis and cardiovascular diseases.

Uses

VX-702 is a third generation inhibitor of p38 mitogen-activated protein (MAP) kinases, binding to both p38α and p38β (Kd = 3.7 and 17 nM, respectively) in an ATP-competitive fashion. It inhibits IL-6, IL-1β, and TNF-α production in LPS-primed blood with IC50 values of 59, 122, and 99 ng/ml, respectively. VX-702, at 1 μM, inhibits activation of p38 in platelets by thrombin, U-46619 , or collagen but does not block platelet aggregation in response to collagen. Although orally active, VX-702 provides only transient suppression of biomarkers of inflammation in ongoing rheumatoid arthritis.[Cayman Chemical]

Definition

ChEBI: 6-(N-carbamoyl-2,6-difluoroanilino)-2-(2,4-difluorophenyl)-3-pyridinecarboxamide is a phenylpyridine.

storage

+4°C

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