VX-702

VX-702 is a third generation inhibitor of p38 mitogen-activated protein (MAP) kinases, binding to both p38alpha and p38beta (Kd = 3.7 and 17 nM, respectively) in an ATP-competitive fashion. It inhibits IL-6, IL-1beta, and TNF-alpha 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 (Cay-16450), 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.Formal Name: 6-[(aminocarbonyl)(2,6-difluorophenyl)amino]-2-(2,4-difluorophenyl)-3-pyridinecarboxamide. CAS Number: 745833-23-2. Molecular Formula: C19H12F4N4O2. Formula Weight: 404.3. Purity: >95%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 3 mg/ml, DMSO: 14 mg/ml, DMSO:PBS(pH 7.2) (1:3): 0.5 mg/ml. lambdamax: 203, 240, 291 nm. SMILES: FC1=CC=CC(F)=C1N(C2=NC(C3=C(F)C=C(F)C=C3)=C(C(N)=O)C=C2)C(N)=O. InChi Code: InChI=1S/C19H12F4N4O2/c20-9-4-5-10(14(23)8-9)16-11(18(24)28)6-7-15(26-16)27(19(25)29)17-12(21)2-1-3-13(17)22/h1-8H,(H2,24,28)(H2,25,29). InChi Key: FYSRKRZDBHOFAY-UHFFFAOYSA-N.