Vx-702 Inhibitor CAS No. 745833-23-2

Cat. No.	Name	Size	Price
KI1067	Vx-702	10 mg	$112
	Vx-702	25 mg	$176
	Vx-702	100 mg	$592
	Vx-702	200 mg	$1072

Chemical Characteristic

Product Name	Vx-702
CAS No.	745833-23-2
Molecular Weight	404.32
Formula	C₁₉H₁₂F₄N₄O₂
Chemical Name	1-(5-carbamoyl-6-(2,4-difluorophenyl)pyridin-2-yl)-1-(2,6-difluorophenyl)urea
Smiles	N(C(=O)N)(c1c(cccc1F)F)c1ccc(c(n1)c1c(cc(cc1)F)F)C(=O)N
Chemical Structure

Biological activities

VX-702 is a highly selective novel p38 MAPK inhibitor. VX-702 binds to its ATP pocket and inhibits the kinase competitively. VX-702 inhibits the C-reactive protein (CRP) response.^[1] VX-702 is developed for the treatment of rheumatoid arthritis and acute coronary syndrome.^[2] VX-702 significantly inhibits LPS-stimulated TNFα, IL-6 and IL-1β production with IC50 of 99 ng/mL, 59 ng/mL, and 122 ng/mL, respectively.^[3] VX-702 at the dose of 1 µM completely inhibits activation of p38 MAPK by thrombin, SFLLRN, AYPGKF, U46619, and collagen.^[4]

References

[1] Damjanov N, et al. 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.Arthritis Rheum. 2009, 60(5): 1232-1241. [2] Ding C. Drug evaluation: VX-702, a MAP kinase inhibitor for rheumatoid arthritis and acute coronary syndrome. Curr Opin Investig Drugs. 2006, 7(11): 1020-1025. [3] Godfrey C, et al. The pharmacokinetics (PK) and pharmacodynamics (PD) of VX-702, a novel, oral P38MAP kinase inhibitor, in healthy volunteers. Clinical Pharmacology & Therapeutics. 2004, 75: P52. [4] Kuliopulos A, et al. Effect of selective inhibition of the p38 MAP kinase pathway on platelet aggregation. Thromb Haemost. 2004, 92(6): 1387-1393.

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