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Enavatuzumab

Product NameEnavatuzumab
CAS1062149-33-0
MF
MW0
EINECS
MOL FileMol File

Chemical Properties

form	Liquid
color	Colorless to light yellow

Usage And Synthesis

Uses

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 [1] [2].

in vivo

Enavatuzumab (10mg/kg; IP; three times per week; 7 doses) shows diverse antitumor activities on different xenograft tumors^[1].

Animal Model:	6-week old SCID mice with SN12C or HCT116 or DLD-1 or A375 tumors^[1]
Dosage:	10mg/kg
Administration:	IP; three times per week; 6 doses (DLD-1 model), 7 doses (SN12C model), 9 doses (A375 or HCT116 model)
Result:	Some TweakR-expressing cells, such as SN12C and A375, were sensitive in vivo and in vitro. Some TweakR-expressing cell lines, such as HCT116 and DLD-1, were not sensitive to enavatuzumab treatment in vivo, though both cell lines were effectively killed via ADCC in vitro. Up-regulated the activation markers on splenocytes in SN12C tumor-bearing mice.

References

[1] Shiming Ye, et al. Enavatuzumab, a Humanized Anti-TWEAK Receptor Monoclonal Antibody, Exerts Antitumor Activity through Attracting and Activating Innate Immune Effector Cells. J Immunol Res. 2017;2017:5737159. DOI:10.1155/2017/5737159
[2] Ludmilla de Plater, et al. Predictive gene signature of response to the anti-TweakR mAb PDL192 in patient-derived breast cancer xenografts. PLoS One. 2014 Nov 6;9(11):e104227. DOI:10.1371/journal.pone.0104227

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