An inhibitor of p38 MAP kinases
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VX-702

Item No. 13108

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
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(Learn about Variance in Solubility)
DMF: 3 mg/mlDMSO: 14 mg/mlDMSO:PBS(pH 7.2) (1:3): 0.5 mg/ml
λmax
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
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $28

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    10 mg

    $50

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    25 mg

    $118

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    Product Description

    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.1 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.1 VX-702, at 1 μM, inhibits activation of p38 in platelets by thrombin, U-46619 (Item No. 16450), or collagen but does not block platelet aggregation in response to collagen.2 Although orally active, VX-702 provides only transient suppression of biomarkers of inflammation in ongoing rheumatoid arthritis.3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Goldstein, D.M., Kuglstatter, A., Lou, Y., et al. Selective p38α inhibitors clinically evaluated for the treatment of chronic inflammatory disorders. J. Med. Chem. 53, 2345-2353 (2010).

    2. Kuliopulos, A., Mohanlal, R., and Covic, L. Effect of selective inhibition of the p38 MAP kinase pathway on platelet aggregation. Thromb. Haemost. 92, 1387-1393 (2004).

    3. Damjanov, N., Kauffman, R.S., and Spencer-Green, G.T. 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. 60(5), 1232-1241 (2009).