Enavatuzumab (PDL192; ABT-361) 是一种人源化 IgG1 单克隆抗体，靶向 TNF 样细胞凋亡弱诱导剂受体 (TWEAK)。TWEAK (Fn14; TNFRSF12A) 是 TWEAK 受体 (TweakR) 的天然配体，可刺激多种细胞反应。Enavatuzumab 通过直接的 TweakR 信号和抗体依赖性细胞介导的细胞毒性 (ADCC) 诱导肿瘤生长抑制。Enavatuzumab 可以主动募集和激活骨髓效应细胞来杀死肿瘤细胞。Enavatuzumab 在体外和体内抑制各种人类 TweakR 阳性癌细胞系和异种移植物的生长。
| 生物活性 | Enavatuzumab (PDL192; ABT-361) is a humanizedIgG1monoclonal antibody targeting the receptor ofTNF-like weak inducer ofapoptosis(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-positivecancercell lines and xenografts in vitro and in vivo[1][2]. |
体外研究
(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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体内研究
(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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| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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