AX-024 (hydrochloride)

AX-024 is an inhibitor of the CD3epsilon-Nck interaction. It binds to the SH3.1 N-terminal domain of Nck1, preventing its binding to the proline-rich sequence of the CD3epsilon subunit of T cells. AX-024 inhibits T cell receptor-triggered T cell activation (IC50 = 1 nM for human T cells) and selectively decreases proliferation of T cells over B cells. It prevents CD4+ T cell and macrophage infiltration to the cerebellum and spinal cord and improves neurological impairments in a MOG35-55 mouse model of experimental autoimmune encephalomyelitis (EAE) when administered at a dose of 10 mg/kg per day for ten days starting on the day of immunization. AX-024 (50 mg/kg) prevents the infiltration of eosinophils, macrophages, and neutrophils into the airway, as well as prevents an increase in IL-4 levels in bronchoalveolar lavage fluid (BALF), in an ovalbumin-sensitized mouse model of allergic airway disease. It does not prevent the memory T cell response to an immunodominant B8R poxvirus antigen peptide or to infection by ectromelia virus (mousepox).Formal Name: 1-[[4-(4-fluorophenyl)-6-methoxy-2H-1-benzopyran-3-yl]methyl]-pyrrolidine, monohydrochloride. CAS Number: 1704801-24-0. Molecular Formula: C21H22FNO2 . HCl. Formula Weight: 375.9. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMSO: soluble. SMILES: COC1=CC=C2C(C(C3=CC=C(F)C=C3)=C(CN4CCCC4)CO2)=C1.Cl. InChi Code: InChI=1S/C21H22FNO2.ClH/c1-24-18-8-9-20-19(12-18)21(15-4-6-17(22)7-5-15)16(14-25-20)13-23-10-2-3-11-23,/h4-9,12H,2-3,10-11,13-14H2,1H3,1H. InChi Key: DGBCIMPGYRVTPD-UHFFFAOYSA-N.