Cetuximab (C225)是一种单克隆抗体,能够抑制 EGFR,SPR 方法测得 Cetuximab 对 EGFR 的 Kd 值为 0.201 nM;Cetuximab 具有高效的抗肿瘤作用。
生物活性 | Cetuximab (C225) is a monoclonal antibody that inhibits epidermal growth factor receptor (EGFR), with a Kd of 0.201 nM for EGFR by SPR. Cetuximab has potent antitumor activity[1]. |
IC50 & Target | | | | | Soluble EGFR | EGFR 0.147 nM (Kd, Fixed A431 cells) | |
体外研究 (In Vitro) | Cetuximab (C225) is a monoclonal antibody that inhibits epidermal growth factor receptor (EGFR), with a Kd of 0.201 nM for soluble EGFR by SPR. Cetuximab also exhibits a Kd of 0.147 nM for EGFR in fixed A431 cells by ELISA[1]. Cetuximab (C225; 30 nM) time-dependently inhibits the proliferation of SCC-1, SCC-11B, SCC-38, and SCC-13Y cells after treatment for 8 d. Cetuximab (30 nM) causes G0/G1 arrest, induces apoptosis, and reduces Rb, p27KIP1, Bcl-2, and Bax expression in SCC-13Y cells. Cetuximab (30 nM) also enhances radiosensitivity and increases radiation-induced apoptosis in SCC-13Y cells[3]. |
体内研究 (In Vivo) | Cetuximab (1?mg/injection) has effect on the tumour volume but the effect is more pronounced on UT-SCC-14 xenografts. In UT-SCC-14 xenografts, Cetuximab treatment significantly reduces the expression of EGFR, pEGFR and Ki67. The MCT1 and GLUT1 expression is significantly decreased in the Cetuximab-treated groups of both cell lines but differences are more pronounced in UT-SCC-14 xenografts[2]. |
Clinical Trial | NCT Number | Sponsor | Condition | Start Date | Phase | NCT04065555 | Presage Biosciences|Takeda | Head and Neck Cancer | October 7, 2020 | Early Phase 1 | NCT00875849 | Centre Antoine Lacassagne | Head and Neck Cancer | March 2008 | Phase 2 | NCT02555644 | Eli Lilly and Company | Head and Neck Neoplasms | February 24, 2016 | Phase 1 | |
分子量 | 145543.35 |
CAS 号 | 205923-56-4 |
中文名称 | 西妥昔单抗 |
SMILES | [Cetuximab] |
储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
参考文献 | [1]. Goldstein NI, et al. Biological efficacy of a chimeric antibody to the epidermal growth factor receptor in a human tumor xenograft model. Clin Cancer Res. 1995 Nov;1(11):1311-8. [2]. Gustafsson H, et al. EPR Oximetry of Cetuximab-Treated Head-and-Neck Tumours in a Mouse Model. Cell Biochem Biophys. 2017 Jul 29. [3]. Huang SM, et al. Epidermal growth factor receptor blockade with C225 modulates proliferation, apoptosis, and radiosensitivity in squamous cell carcinomas of the head and neck. Cancer Res. 1999 Apr 15;59(8):1935-40. |