VX-702

CHF 60.00
In stock
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Product Details
Synonyms VX702
Product Type Chemical
Properties
Formula C19H12F4N4O2
MW 404.3
CAS 745833-23-2
Purity Chemicals ≥95%
Appearance Solid.
Solubility Soluble in DMSO or ethanol.
Declaration Manufactured by SynKinase.
Other Product Data Target: P38 | Kinase Group: CMGC | Substrate: Serine-Threonine

Click here for Original Manufacturer Product Datasheet
Our product description may differ slightly from the original manufacturers product datasheet.
InChi Key FYSRKRZDBHOFAY-UHFFFAOYSA-N
Shipping and Handling
Shipping AMBIENT
Short Term Storage +4°C
Long Term Storage -20°C
Use/Stability Stable for at least 2 years after receipt when stored at -20°C.
Documents
MSDS Download PDF
Product Specification Sheet
Datasheet Download PDF
The kinases called p38 MAP kinases (MAPKs) are intracellular, soluble serine-threonine kinases which belong to a large family of proteins that include the extracellular regulated kinases (ERKs) and c-Jun N-terminal kinases (JNKs). So far four p38 isoforms have been identified, namely p38α, p38β, p38γ and p38δ , a.k.a., p38-α (MAPK14), -β (MAPK11), -γ (MAPK12 / ERK6), and -δ (MAPK13 / SAPK4). The ubiquitously expressed s p38α has been the most extensively studied and is believed to be the most physiologically relevant in the regulation of the inflammatory response. The role of the three other isoforms is not currently well understood, however their primary sites of expression are known. Similar to p38α, p38β is also ubiquitously expressed, while p38γ is expressed predominately in skeletal muscle and p38δ is expressed primarily in the lung, kidney, testis, small intestine and pancreas. The small molecule inhibitor VX-702 is a potent p38 kinase family inhibitor that has been studied for its effects on inflammation and the inflammatory response. VX-702 dose-dependently inhibited the production o IL-6, IL-1β and TNFα (IC(50) = 59, 122 and 99ng/ml, respectively), and in anti-platelet aggregation assays, pre-incubation of platelets with VX-702 (1µM)completely or partially inhibited platelet agonist induced p38 activation (IC(50) = 4 to 20nM). More recently VX-702 has been studied as a potential treatment for rheumatoid arthritis (RA). VX-702 appears to be most effective against MAPK14, followed by MAPK11 and the remaining members of the family, however exact in vitro IC(50) values have not been published. However a large amount of data is available for in vitro growth inhibition assays where VX-702 exhibits poptent activity , having low IC(50) values beginning at ~16nM and ending at < 400µM for the numerous cell lines tested.
Product References
  1. Effect of selective inhibition of the p38 MAP kinase pathway on platelet aggregation: A. Kuliopulos, et al.; Thromb. Haemost. 92, 1387 (2004)
  2. Drug evaluation: VX-702, a MAP kinase inhibitor for rheumatoid arthritis and acute coronary syndrome: C. Ding; Curr. Opin. Investig. Drugs 7, 1020 (2006)
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