AX-024 | Inhibitor of T cell antigen receptor (TCR)-dependent T cell activation

CAS:
1704801-24-0
Catalog Number:
10-4895
Activity:
Inhibitor of T cell antigen receptor (TCR)-dependent T cell activation
Chemical Name:
1-[[4-(4-Fluorophenyl)-6-methoxy-2H-chromen-3-yl]methyl]pyrrolidine hydrochloride
Molecular Weight:
375.86
Molecular Formula:
C21H22FNO2•HCl
Solubility:
Soluble in DMSO (up to at least 25 mg/ml with warming) or in Water (10 mg/ml with warming).
Physical Properties:
White solid
Purity:
98% by HPLC
NMR (Conforms)
Storage Temperature:
-20°
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.
Shipping Code:
RT

Available Options

Size:PriceQuantity 
5 mg$90.00
25 mg$330.00

AX-024 (1704801-24-0) is a potent (IC50 ~ 1 nM) and specific inhibitor of T cell antigen receptor (TCR)-dependent T cell activation. It inhibited neither B cell proliferation triggered by B cell antigen receptor (BCR), TLR4, CD40 agonists nor IL-2-dependent proliferation of T lymphoblasts. AX-024 binds to the SH3.1 domain of the adaptor protein Nck blocking its interaction with the CD3e subunit on the T cell antigen receptor. AX-024 displayed protective effects in mouse models of psoriasis, allergic asthma, and multiple sclerosis. Importantly, the therapeutic effect of AX-024 persisted after removal of the drug in contrast to fingolimod suggesting a persistent modification of autoimmune T cells. Currently in clinical trials.

References/Citations:

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

CAS:
1704801-24-0
Catalog Number:
10-4895
Activity:
Inhibitor of T cell antigen receptor (TCR)-dependent T cell activation
Chemical Name:
1-[[4-(4-Fluorophenyl)-6-methoxy-2H-chromen-3-yl]methyl]pyrrolidine hydrochloride
Molecular Weight:
375.86
Molecular Formula:
C21H22FNO2•HCl
Solubility:
Soluble in DMSO (up to at least 25 mg/ml with warming) or in Water (10 mg/ml with warming).
Physical Properties:
White solid
Purity:
98% by HPLC
NMR (Conforms)
Storage Temperature:
-20°
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.
Shipping Code:
RT

Safety Data Sheet:

N/A

Product Data Sheet:

Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications. Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee