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Cetuximab (C225) (Synonyms: C225)

Katalog-Nr.GC34217

Cetuximab (C225) ist ein humaner IgG1-Monoklonaler Antikörper, der den epidermalen Wachstumsfaktorrezeptor (EGFR) hemmt, mit einem Kd von 0,201 nM für EGFR durch SPR. Cetuximab (C225) hat eine starke antitumorale Aktivität.

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Cetuximab (C225) Chemische Struktur

Cas No.: 205923-56-4

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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Protocol

Cell experiment [1]:

Cell lines

SCC1 and UM-SCC-22B cells

Preparation Method

The toxicity of cetuximab to SCC1 and UM-SCC-22B cells was determined by MTT assay. At 72 h or 120 h after treatment with different doses of cetuximab (ranging from 0.1 nM to 0.5 μM), the culture medium was replaced and 50 μl of 1.0 mg/ml sterile filtered 3-(4, 5-dimethylthiazol-2-yl)-2, 5-diphenyl tetrazolium bromide (MTT; Sigma) was added to each well.

Reaction Conditions

0.1 nM to 0.5 μM at 72 h or 120 h

Applications

Treatment with cetuximab produced only modest inhibition of cell proliferation on SCC1 cells in vitro as determined by MMT assay.

Animal experiment [2]:

Animal models

BALB/c (nu/nu) female nude mice

Preparation Method

Xenografts were established in female nude mice (BALB c[nu/nu]) by subcutaneous injection of head and neck squamous cell carcinoma cell lines a UT-SCC-14 and b UT-SCC-2. Cetuximab (1 mg/injection) was administered by intraperitoneal injection at day 10, 13 and 16. The tumour size was recorded at an interval of 2–3 days, n = 10-14.

Dosage form

1 mg, i.p.

Applications

Cetuximab treatment showed reduction in the nuclear accumulation of HIF-1α, while the overall HIF-1α expression was not significantly altered. And after cetuximab treatment a downregulation of CAIX was only found in UT-SCC-14 xenografts. Cetuximab treatment affects the tumour growth and the tumour partial oxygen pressure as measured by LiPc EPR oximetry.

References:

[1]. Niu G, et al. Cetuximab-based immunotherapy and radioimmunotherapy of head and neck squamous cell carcinoma. Clin Cancer Res. 2010 Apr 1;16(7):2095-105.

[2]. Gustafsson H, et al. EPR Oximetry of Cetuximab-Treated Head-and-Neck Tumours in a Mouse Model. Cell Biochem Biophys. 2017 Dec;75(3-4):299-309.

Background

Cetuximab ist ein chimärer monoklonaler Antikörper, der durch Fusion des variablen Bereichs des murinen Anti-EGFR-Monoklonalantikörpers M225 und des menschlichen IgG1-Konstantbereichs erzeugt wurde. Der produzierte Antikörper behält eine hohe Affinität und Spezifität für EGFR bei und reduziert die Immunogenität.[1] Cetuximab bindet mit hoher Affinität an FcγRI (EC50 = 0,13 nM) und FcγRIIIa (EC50 = 6 nM). Es induziert effektiv ADCC über mehrere Tumorzelllinien hinweg.[4] Die Behandlung mit 100 μg/ml Cetuximab für 24 Stunden verstärkt den zytotoxischen Effekt der RSL3-Behandlung auf KRAS-mutierte CRC-Zellen.[2]

Ein In-vitro-Experiment zeigte, dass Strahlung die cetuximab (0,5 μg/ml)-vermittelte ADCC und Aktivierung von NK-Zellen verstärkt. Die Behandlung mit 20 μg/mL Cetuximab hemmte die Proliferation der Elternzelllinie UMSCC1 (UMSCC1-P), während die drei HNSCC-Cetuximab-resistenten Klone (C2, C5 und C11) vollständig gegenüber Cetuximab unempfindlich waren.

Im In-vivo-Experiment wurde gezeigt, dass Cetuximab (13 mg/kg, s.c.) die hemmenden Wirkungen von RSL3 und RSL3-induzierter Ferroptose verstärkt.[2] Im In-vivo-Versuch zeigte sich nach i.v.-Injektion von 4 Dosen zu je 10 mg/kg Körpergewicht, dass Cetuximab das Tumorwachstum bei Mäusen mit SCC1-Tumoren deutlich hemmt.[5] Im In-vivo-Experiment wurde veranschaulicht, dass durch Behandlung mit Cetuximab (50 mg/kg, i.p.) das Tumorwachstum verzögert wird, wenn Mäuse individuell mit 2x106 Tumorzellen der NSCLC H226-Zelllinie im dorsalen Flankenbereich inokuliert wurden.[6]

References:
[1]. Xiong HQ, et al. Cetuximab, a monoclonal antibody targeting the epidermal growth factor receptor, in combination with gemcitabine for advanced pancreatic cancer: a multicenter phase II Trial. J Clin Oncol. 2004 Jul 1;22(13):2610-6.
[2]. Yang J, et al. Cetuximab promotes RSL3-induced ferroptosis by suppressing the Nrf2/HO-1 signalling pathway in KRAS mutant colorectal cancer. Cell Death Dis. 2021 Nov 13;12(11):1079.
[3]. Jin WJ, et al. Tumor-Specific Antibody, Cetuximab, Enhances the In Situ Vaccine Effect of Radiation in Immunologically Cold Head and Neck Squamous Cell Carcinoma. Front Immunol. 2020 Nov 12;11:591139.
[4]. Patel D, et al. IgG isotype, glycosylation, and EGFR expression determine the induction of antibody-dependent cellular cytotoxicity in vitro by cetuximab. Hum Antibodies. 2010;19(4):89-99.
[5]. Niu G, et al. Cetuximab-based immunotherapy and radioimmunotherapy of head and neck squamous cell carcinoma. Clin Cancer Res. 2010 Apr 1;16(7):2095-105.
[6]. Iida M, et al. Targeting the HER Family with Pan-HER Effectively Overcomes Resistance to Cetuximab. Mol Cancer Ther. 2016 Sep;15(9):2175-86.

Chemical Properties

Cas No. 205923-56-4 SDF
Überlieferungen C225
Canonical SMILES [Cetuximab]
Formula C6484H10042N1732O2023S36 M.Wt 145543.35
Löslichkeit Storage Store at 4°C, do not freeze
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

Prepare stock solution
1 mg 5 mg 10 mg
1 mM 0.0069 mL 0.0344 mL 0.0687 mL
5 mM 0.0014 mL 0.0069 mL 0.0137 mL
10 mM 0.0007 mL 0.0034 mL 0.0069 mL
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Average Rating: 5 ★★★★★ (Based on Reviews and 24 reference(s) in Google Scholar.)

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