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ALX-430-096 [ALEXIS] Revised 24-Feb-05
A77 1726 SYNONYMS    N-(4-Trifluoromethylphenyl)-2-cyano-3-hydroxycrotonamide 2-Cyano-3-hydroxy-N-[4-(trifluoromethyl)phenyl]-2-butenamide PRODUCT LINE    Signal Transduction PRODUCT FAMILIES    Tyrosine Kinase Inhibitors Ordering Information  Product Numbers Format Size Unit Price Quantity  ALX-430-096-M005 5 mg      ALX-430-096-M025 25 mg     Product Specification FORMULA:    C12H9F3N2O2   MW:    270.2   CAS NUMBER:    108605-62-5   PURITY:    ≥98%   APPEARANCE:    White solid.   SOLUBILITY:    Soluble in DMSO.   SHIPPING:    AMBIENT   LONG TERM STORAGE:    +4°C   HANDLING:    Protect from light. Keep under inert gas. Product Description Physiologically active metabolite of the immunosuppressive drug leflunomide (Prod. No. ALX-430-095). Inhibits the activity of dihydrorotate dehydrogenase and of protein tyrosine kinases. Blocks TNF-mediated NF-κB activation in a dose- and time-dependent manner. Also inhibits the activity of cyclooxygenase-2 (COX-2) in vitro and in vivo. Product Specific Literature References Inhibition of the epidermal growth factor receptor tyrosine kinase activity by leflunomide: T. Mattar, et al.; FEBS Lett. 334, 161 (1993) Abstract Inhibition of protein tyrosine phosphorylation in T cells by a novel immunosuppressive agent, leflunomide: X. Xu, et al.; J. Biol. Chem. 270, 12398 (1995) Full Text; http://www.jbc.org/cgi/reprint/270/21/12398 The immunosuppressive metabolite of leflunomide is a potent inhibitor of human dihydroorotate dehydrogenase: J.P. Davis, et al.; Biochemistry 35, 1270 (1996) Abstract Two activities of the immunosuppressive metabolite of leflunomide, A77 1726. Inhibition of pyrimidine nucleotide synthesis and protein tyrosine phosphorylation: X. Xu, et al.; Biochem. Pharmacol. 52, 527 (1996) Abstract The immunosuppressive metabolite of leflunomide, A77 1726, affects murine T cells through two biochemical mechanisms: R.T. Elder, et al.; J. Immunol. 159, 22 (1997) Abstract In vivo mechanism by which leflunomide controls lymphoproliferative and autoimmune disease in MRL/MpJ-lpr/lpr mice: X. Xu, et al.; J. Immunol. 159, 167 (1997) Abstract Immunosuppressive leflunomide metabolite (A77 1726) blocks TNF-dependent nuclear factor-kappa B activation and gene expression: S.K. Manna & B.B. Aggarwal; J. Immunol. 162, 2095 (1999) Abstract A771726, the active metabolite of leflunomide, directly inhibits the activity of cyclo-oxygenase-2 in vitro and in vivo in a substrate-sensitive manner: L.C. Hamilton, et al.; Br. J. Pharmacol. 127, 1589 (1999) Abstract RELATED PRODUCT GROUPS    Immunology > Immunomodulators > Immunomodulators Other Products / Signal Transduction > NF-kB Pathway > NF-kB Pathway Inhibitors / Inflammation > Cyclooxygenases [COX] / Related Products > COX Inhibitors