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Other Sizes |
Cetuximab (C225; C 225; C-225; Erbitux) is a potent and specific chimeric monoclonal antibody approved for cancer treatment. It inhibits epidermal growth factor receptor (EGFR) with a Kd of 0.201 nM for soluble EGFR by SPR. Cetuximab has potent antitumor activity and has been approved for use in the treatment of metastatic colorectal cancer, metastatic non-small cell lung cancer and head and neck cancer. Cetuximab is a chimeric (mouse/human) monoclonal antibody given by intravenous infusion that is distributed under the trade name Erbitux in the U.S. and Canada by the drug company Eli Lilly and Co. and outside those countries by the drug company Merck KGaA. In Japan, Merck KGaA, Bristol-Myers Squibb and Eli Lilly have a co-distribution.
ln Vitro |
With an SPR Kd of 0.201 nM for soluble EGFR, cetuximab (C225) is a monoclonal antibody that suppresses the epidermal growth factor receptor (EGFR). The Kd of cetuximab for EGFR in fixed A431 cells was likewise 0.147 nM as shown by ELISA detection [1]. After 8 days of therapy, the proliferation of SCC-1, SCC-11B, SCC-38, and SCC-13Y cells is time-dependently inhibited by cetuximab (C225; 30 nM). In SCC-13Y cells, cetuximab (30 nM) promotes apoptosis, causes G0/G1 arrest, and lowers the expression of Rb, p27KIP1, Bcl-2, and Bax. In SCC-13Y cells, cetuximab (30 nM) also accelerates radiation-induced apoptosis and increases radiosensitivity [3].
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ln Vivo |
Tumor volume was impacted by cetuximab (1 mg/injection), while the impact was more in UT-SCC-14 xenografts. In UT-SCC-14 xenografts, cetuximab markedly decreased the expression of EGFR, pEGFR, and Ki67. In MCT1 and GLUT1 cells, cetuximab markedly decreased expression; however, in UT-SCC-14 xenografts, the difference was more noticeable [2].
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Animal Protocol |
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References |
[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. |
Molecular Formula |
C6484H10042N1732O2023S36
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Molecular Weight |
145781.92
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CAS # |
205923-56-4
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SMILES |
Br.OC(CCCCCN1C(=C)C(C)(C)C2=CC=CC=C12)=O
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Synonyms |
Cetuximab (anti-EGFR) IMC 225 Hsdb 7454CETUXIMAB EGFR antibody Unii-pqx0D8J21jCETUXIMAB USP/EP/BP CetuxiMab(C225)Immunoglobulin G1, anti-(human epidermal growth factor receptor) (human-mouse monoclon
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 :Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400  (Please use freshly prepared in vivo formulations for optimal results.) |
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Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 0.0069 mL | 0.0343 mL | 0.0686 mL | |
5 mM | 0.0014 mL | 0.0069 mL | 0.0137 mL | |
10 mM | 685.9562 nL | 0.0034 mL | 0.0069 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.