CTX-471

Names

[ CAS No. ]:
2377152-49-1

[ Name ]:
CTX-471

Biological Activity

[Description]:

CTX-471 is a fully human monoclonal antibody of CD137. CTX-471 has bind affinity for recombinant human, cynomolgus macaque CD137 and mouse CD137 with Kd values of 50 nM, 61 nM and 748 nM, respectively. CTX-471 can be used for the research of immunomodulation and cancer[1].

[Related Catalog]:

Research Areas >> Cancer
Signaling Pathways >> Immunology/Inflammation >> Interleukin Related
Research Areas >> Inflammation/Immunology

[Target]

Kd for CD137: 50 nM (human); 61 nM (cynomolgus macaque); 748 nM (mouse)[1]


[In Vitro]

CTX-471 (5-500 nM) has bind affinity for recombinant human, cynomolgus macaque CD137 and mouse CD137 with Kd values of 50 nM, 61 nM and 748 nM, respectively[1]. CTX-471 binds to a unique epitope on CD137[1]. CTX-471 (0.1-100 nM; 1, 10 μg/mL; 3 days) increases IFN-y production by human T cells in an Fcy receptor-dependent (FcyR-dependent) manner in vitro[1].

[In Vivo]

CTX-471 (i.p.; 150 μg) exhibits curative monotherapy activity in various syngeneic tumor models and shows a unique ability to cure mice of very large tumors.CTX-471 (i.v.; 10-80 mg/kg; on days 0, 7, 14, and 21) is well tolerated, with no signs of hepatic toxicity in high doses. Animal Model: BALB/c mice[1] Dosage: 150 μg; 10-80 mg/kg Administration: i.p., on days 6, 9, 12, 19 and 26( or on days 7, 10, 13, 20, and 27 or on days 0, 3, 6, and 9); i.v., on days 0, 7, 14, and 21 Result: Required T and NK cells, as well as FcγR engagement to achieve its efficacy. Do not induce hepatic inflammation.

[References]

[1]. Ugur Eskiocak, et al. Differentiated agonistic antibody targeting CD137 eradicates large tumors without hepatotoxicity. JCI Insight. 2020 Mar 12;5(5):e133647.

Chemical & Physical Properties

[ Molecular Formula ]:
CT


Related Compounds