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西妥昔单抗Cetuximab (anti-EGFR) 205923-56-4

  • 价  格:¥11985
  • 货  号:205923-56-4
  • 产  地:北京
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产品描述 Cetuximab (anti-EGFR)是一种新型的分子靶向药物,是EGFR的抑制剂,同时也是人源EGFR单克隆抗体,与EGFR的胞外结合区域相互作用并抑制其受配体刺激;MW:145.781 KD。
靶点
EGFR [4]
(Cell-free assay)
0.39 nM(Kd)
体外研究

Cetuximab (anti-EGFR)是一种重组嵌合的单克隆抗体,与人类EGFR受体具有高度亲和力。它与EGFR结合、抑制其受体相关的激酶的磷酸化合激活,从而导致细胞生长受到抑制、诱导细胞凋亡并减少VEGF的产生[5]。Cetuximab具有显著的单药抗肿瘤作用,在高表达EGFR蛋白的NPC细胞系中与cisplatin或paclitaxel具有加成作用,但对低表达EGFR的NPC细胞系(如CNE-2和C666-1)的作用甚微[1]。Cetuximab阻止EGFR与配体的相互作用,抑制下游RAS-ERK激活。它能够促进内质网应激反应(ER stress),促使ER蛋白转运至细胞膜。它竞争性地抑制配体结合,抑制酪氨酸激酶激活,导致受体下调。除了竞争性抑制作用,cetuximab与EGFR结合还可能引起受体内在化和被破坏[3]。

体内研究

在小鼠移植瘤模型中,Cetuximab能够增强几种化疗药物的抗肿瘤活性[1]。它通过多种机制,包括抑制细胞周期的进展,将细胞周期阻滞在G1期、减少S期细胞数目来发挥其抗肿瘤作用。Cetuximab将细胞阻滞在G1期还能引起凋亡,通过诱导和激活相关促凋亡分子。单独给药或是与carboplatin协同给药能够引起肿瘤大小减少、转移扩散减少、减少细胞表面表达EGFR、无BRAF和K-ras突变的NCI-N87肿瘤中MVD。而在源自于MKN-45的肿瘤中作用甚微(其肿瘤表型是BRAF和K-ras行盛行,但胞质内EGFR弱表达)[3]。
细胞实验: - 合并

Objective: 细胞活力检测
Cells: HNE1和CNE2细胞
Concentrations: 62.5, 125, 250, 500, 1000 或 2000 µg/ml
Incubation Time: 48 h
Method: 将细胞以5 × 103个细胞/孔的密度培养与平底96孔板。在37℃、5% CO2的条件下孵育24小时后,将200 μL用培养基稀释成不同浓度的cetuximab (62.5, 125, 250, 500, 1000或2000 µg/mL)和/或cisplatin (0.25, 0.5, 1, 2, 4或8 µg/mL)加入每孔。处理48小时后,向每孔加入10 μL CCK-8。孵育2小时后,通过检测450 nm处的吸收光值检测细胞活力。
Reference: https://www.ncbi.nlm.nih.gov/pubmed/27313893

Objective: To analyze the apoptosis of CRC cells
Cells: human DiFi CRC (Colorectal Cancer) cells
Concentrations: 10 μg/ml
Incubation Time: 72h
Method: To analyze the apoptosis, cells were seeded into 6-well plates (3 × 105 cells per well). After 24 h, cells were cultured both in the absence and presence of drugs. Cell death and apoptosis were assessed by cytofluorimetric analysis using PE-annexin V and 7-aminoactinomycin D (7-AAD) according to the manufacturer's instructions at different time points.
Reference: https://www.ncbi.nlm.nih.gov/pubmed/27135741

Cetuximab can apply to nude mice, various cancer cell lines and other related assays (Only for Reference)

动物实验: - 合并

Objective: Cetuximab在小鼠胃癌模型中的抗肿瘤活性
Animal Models: 人类胃癌的裸鼠模型(CD-1/nu-nu mice)
Formulation: 0.9% NaCl
Dosages: 1 mg/kg
Administration: i.p.
Reference: https://www.ncbi.nlm.nih.gov/pubmed/22011788

Objective: To investigate the relationship between the EGFR levels and the responsiveness to cetuximab treatment in human cancer xenograft models
Animal Models: Female athymic, nude mice were implanted s.c. with ~1 mm3 tumor fragments
Formulation: PBS
Dosages: 0.25, 0.5 or 1 mg/mouse
Administration: i.p.
Reference: https://www.ncbi.nlm.nih.gov/pubmed/27186886

Cetuximab can apply to nude mice, various cancer cell lines and other related assays (Only for Reference)

参考文献

[1] Gu J, et al. Biochem Res Int. 2016, 2016:7016907.
[2] Pozzi C, et al. Nat Med. 2016, 22(6):624-31.
[3] Hotz B, et al. Gastric Cancer. 2012, 15(3):252-64.

[4] Kim GP, et al. Biologics. 2008, 2(2):223-8.

- 合并
抗体信息
CAS No. 205923-56-4
Formulation PBS buffer, pH 7.2
Isotype Human IgG1
Source CHO cells
Storage Store the undiluted solution at 4°C in the dark to avoid freeze-thaw cycles

单抗药物对照品
贝伐单抗,Bevacizumab 纳武单抗,Nivolumab
帕妥珠单抗,Pertuzumab 曲妥珠单抗,Trastuzumab
阿达木单抗,Adalimumab 帕姆单抗,Pembrolizumab
迪诺苏单抗,Denosumab 阿替唑单抗,Atezolizumab
优特克诺单抗,Ustekinumab 维多珠单抗,Vedolizumab
1、33个产品,三种规格:1mg,2mg,5mg;
2、价格优,全现货;
3、科研产品,仅用科研,禁用临床;

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