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1704801-24-0

1704801-24-0 Structure

1704801-24-0 Structure
IdentificationBack Directory
[Name]

AX-024 hydrochloride
[CAS]

1704801-24-0
[Synonyms]

AX-024
AX-024;AX024;AX 024
AX-024 hydrochloride
[Molecular Formula]

C21H23ClFNO2
[MDL Number]

MFCD31628548
[MOL File]

1704801-24-0.mol
[Molecular Weight]

375.87
Chemical PropertiesBack Directory
[storage temp. ]

-20°
[solubility ]

Soluble in DMSO (up to at least 25 mg/ml with warming) or in Water (10 mg/ml with warming).
[form ]

solid
[color ]

White
[Stability:]

Stable for 1 year from date of purchase as supplied. Solutions in DMSO or distilled water may be stored at -20° for up to 3 months.
Safety DataBack Directory
[Symbol(GHS) ]


GHS07
[Signal word ]

Warning
[Hazard statements ]

H302-H315-H319-H335
[Precautionary statements ]

P261-P305+P351+P338
Hazard InformationBack Directory
[Description]

AX-024 is an inhibitor of the CD3ε-Nck interaction. It binds to the SH3.1 N-terminal domain of Nck1, preventing its binding to the proline-rich sequence of the CD3ε 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).
[Uses]

AX-024 is a T cell receptor inhibitor for the treatment of autoimmune diseases.
[References]

1) Borroto et al. (2016), First-in-class inhibitor of the T cell receptor for the treatment of autoimmune diseases; Sci. Transl. Med., 8 370ra184
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