| Description |
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].
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| Related Catalog |
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| In Vitro |
Enavatuzumab (0.1-1000 ng/mL; 4 小时) 在体外诱导效应细胞活化和肿瘤细胞杀伤[1]。 Enavatuzumab (10μg/mL; 24 小时) 导致免疫效应细胞向 SN12C 和 A375 肿瘤细胞的迁移显着增加[1]。 Cell Viability Assay[1] Cell Line: Renal carcinoma cell line SN12C, the melanoma cell line A375, the colorectal cancer cell lines HCT116 and DLD-1 Concentration: 0.1, 1, 10, 100, 1000 ng/mL Incubation Time: 4 hours Result: Showed potent tumor cell killing on all TweakR-positive tumor cells tested.
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| In Vivo |
Enavatuzumab (10mg/kg; 腹腔注射; 每周 3 次; 6, 7 或者 9 剂) 对不同的异种移植肿瘤表现出不同的抗肿瘤活性[1]。 Animal Model: 6-week old SCID mice with SN12C or HCT116 or DLD-1 or A375 tumors[1] Dosage: 10 mg/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.
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| 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. [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.
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