TNFRSF12A/TWEAK Inhibitor

Enavatuzumab (PDL192; ABT-361) is a humanized IgG1 monoclonal antibody targeting the receptor of TNF-like weak inducer of apoptosis (TWEAK). TWEAK (Fn14; TNFRSF12A), the natural ligand of the TWEAK receptor (TweakR), stimulates multiple cellular responses. Enavatuzumab induces tumor growth inhibition through direct TweakR signaling and antibody dependent cell-mediated cytotoxicity (ADCC). Enavatuzumab can actively recruits and activates myeloid effectors to kill tumor cells. Enavatuzumab inhibits the growth of various human TweakR-positive cancer cell lines and xenografts in vitro and in vivo .

L524-0366 is a specific, dose-dependent TWEAK-Fn14 inhibitor. L524-0366 specifically binds to the Fn14 surface with a K_D of 7.12 μM, competitively inhibiting the binding of Fn14 to TWEAK (inhibition rate reaching 16%). L524-0366 inhibits TWEAK-induced glioma cell migration without potential cytotoxic effects.

RG-7212 (RO5458640) is a human-derived antibody expressed in CHO cells, targeting TNFSF12/TWEAK. RG-7212 (RO5458640) has a huIgG1 type heavy chain and a huκ type light chain, with a predicted molecular weight (MW) of 146.02 kDa. The isotype control for RG-7212 (RO5458640) can be referenced as Human IgG1 kappa, Isotype Control (HY-P99001).