GC1118
Based on 1 Customer Validation
GC1118 (GC-1118A) is a fully human anti-EGFR monoclonal antibody with binding affinity of 0.16 nM (KD) to EGFR. GC1118 displays potent inhibitory effects on high- and low-affinity EGFR ligand-induced signaling. GC1118 shows potent anti proliferative activity in KRAS wild-type and KRAS mutant cells. GC1118 can reach the tumor by crossing both BBB (blood-brain barrier) and BTB (brain-tumor barrier) and shows superior anti-tumor effects in various mice xenograft models. GC1118 can be used for the researches of cancer, such as colorectal cancer.
For research use only. We do not sell to patients.
- Purity : 99.22%
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
All EGFR Isoforms
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Biological Activity
Description
Species Reactivity
Human
IC50 & Target
EGFR
In Vitro
GC1118 (GC-1118A) (1 μg/mL, 24-120 h) shows potent anti proliferative activity in KRAS wild-type and KRAS mutant cells[1][4].
GC1118 (100 µM, 6 days) suppresses cell growth in PDCs of G096 and G022[2].
GC1118 (0.1-50 μg/mL, 2 h) blocks EGFR high- and low-affinity ligand-induced EGFR signaling in HCT8 cells[3].
GC1118 (0.005-100 μg/mL, 3 days) inhibits high- and low-affinity ligand-induced proliferation in HCT8 cells[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:SNU-1, SNU-5, SNU-16, SNU-216, SNU-484, SNU-601, SNU-620, SNU-638, SNU-668, SNU-719, AGS, MKN-45 and NCI-N87 cells
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Concentration:0, 0.001, 0.01, 0.1, 1, 10, 100 and 1000 µg/ mL
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Incubation Time:72 h
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Result:Suppressed cell growth, particularly in the MKN-45 cell line.
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Cell Line:SNU-484, SNU-601, SNU-719 and MKN-45 cells
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Concentration:1 µg/mL
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Incubation Time:24, 72, 120 h
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Result:Showed more obviously anti-growth inhibitory effect in KRAS wild-type cell lines, SNU-719 and MKN-45, but also in KRAS mutant SNU-601 cells.
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Cell Line:HCT8 cells
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Concentration:0.1, 0.5, 5 and 50 μg/mL
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Incubation Time:2 h, stimulated with EGFR ligands (250 ng/mL EGF, HB-EGF, BTC, and TGF-α; 300 ng/mL AREG; 500 ng/mL EREG)
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Result:Inhibited the high- and low-affinity ligand-induced Y1068 phosphorylation, Akt and Erk levels.
In Vivo
GC1118 (GC-1118A) (1 mg/kg, i.p., twice a week for 5 weeks) significantly suppresses xenograft tumor growth in AGS xenograft mice models[1].
GC1118 (50 mg/kg, i.p., twice a week) shows superior antitumor activity in patient-derived GBM xenograft models[2].
GC1118 (1 mg/mouse, i.p., twice a week for 5 weeks) significantly suppresses the tumor growth in HCT8, Lovo, HCT15, LS174T, LS513, and SW48 xenograft mice models[3].
GC1118 (1 mg/mouse, i.p., twice a week for 52 days) had moderate antitumor effects in CRC-024T patient-derived xenograft mice models[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:AGS xenograft mice models (athymic nude mice, female, 6 weeks, tumor volume of 200 mm3)[1]
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Dosage:1 mg/kg
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Administration:Intraperitoneally injection, twice a week for 5 weeks
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Result:Showed a significant suppression of the tumor growth.
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Animal Model:Patient-derived GBM xenograft models (BALB/c nude mice, female, 6-8 weeks, tumor volume of 150-200 mm3)[2]
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Dosage:50 mg/kg
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Administration:Intraperitoneal injection; twice a week until euthanasia
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Result:Exerted anti-tumor effects in eight PDXs (G022, G677, B802, G608, G542, G096, G698, and G500).
Showed significantly better survival outcome than the control group.
Showed a significant amount accumulated in the tumor core.
Significantly increased tumor cell apoptosis and reduced microvascular density (MVD).
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Animal Model:HCT8, Lovo, HCT15, LS174T, LS513, and SW48 xenograft mice models (athymic nude mice, 7-8 weeks, tumor volume of 200 mm3)[3]
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Dosage:1 mg/mouse
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Administration:Intraperitoneally injection, twice a week for 5 weeks
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Result:Significantly suppressed the tumor growth.
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Animal Model:CRC-024T patient-derived xenograft mice models (BALB/c-nude mice, female, 6-8 weeks, tumor volume of 200-250 mm3)[4]
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Dosage:1 mg/mouse
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Administration:Intraperitoneally injection, twice a week for 52 days
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Result:Had moderate antitumor effects and no reduction in body weight.
Downregulated the levels of AKT and ERK1/2.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Gene ID
Accession
P00533-1
Conjugated
Unconjugated
Reconsititution
The product can be reconstituted/diluted with sterile PBS or saline.
Application
ELISA, FACS, Functional assay
Verified Bioactivity
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Immobilized EGFR-his can bind GC1118. The EC50 for this effect is 9.234 ng/mL.
Chemical Information
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Appearance Liquid
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Color Colorless to light yellow
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SMILES
N/A
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Synonyms
GC-1118A
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Shipping
Shipping with dry ice.
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Formulation
Please refer to the lot-specific COA for specific buffer information.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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Patient-Derived Xenograft (PDX)
Patient-derived xenograft (PDX) models are generated by engrafting primary human tumor tissue directly into immunodeficient mice, allowing in vivo propagation of patient tumor biology without initial in vitro adaptation. These models are used to preserve key histopathological and molecular characteristics of the original tumor and enable assessment of tumor growth dynamics and therapeutic response in a living organism. The biological readout is tumor engraftment and subsequent growth in the murine host, which reflects the ability of human tumor cells to survive, vascularize, and expand in an immunocompromised microenvironment.
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Splenic/Portal-Vein Liver Metastasis Xenograft
Splenic and portal-vein liver metastasis xenograft models deliver tumor cells into the portal circulation so that cells reach the liver first and form hepatic metastatic lesions; splenic injection uses the spleen as an access route to the portal system, while direct portal-vein injection introduces cells into the portal vein without requiring splenectomy. The assay detects liver colonization, intrahepatic tumor growth, tumor distribution, treatment response, survival, and liver-metastasis microenvironment changes; readouts include bioluminescence or fluorescence imaging, gross liver nodule counts, liver weight or tumor burden, histology, and survival.
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Subcutaneous Cell-Line-Derived Xenograft
Subcutaneous cell-line-derived xenograft (CDX) models are established by implanting cultured human cancer cell lines into immunodeficient mice, where the injected cells form localized tumors that can be monitored in vivo as a measure of tumorigenic potential, growth kinetics, and treatment response. These models are widely used in oncology research because they allow reproducible tumor formation and enable comparative assessment of tumor growth between different cell lines or genetic manipulations in a controlled in vivo microenvironment. Subcutaneous implantation of cancer cells in immunodeficient mice is a standard approach for evaluating tumor growth behavior and therapeutic response across multiple cancer types, including prostate, esophageal, pancreatic, and colon cancer models.
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Orthotopic Cell-Line Xenograft
Orthotopic cell-line xenograft models involve implantation of human cancer cell lines into the anatomically corresponding organ of immunodeficient mice to reproduce tumor growth within a native microenvironment, enabling more clinically relevant tumor behavior compared with subcutaneous models. These models are widely used because orthotopic placement better recapitulates tumor progression, including invasion and metastatic spread, which are often underrepresented in heterotopic implantation systems. Compared with conventional xenografts, orthotopic implantation is described as more technically complex but provides improved simulation of tumor-microenvironment interactions and metastatic behavior, making it particularly valuable for translational oncology research. Surgical orthotopic implantation approaches have been emphasized as enabling faithful reproduction of clinical cancer features, including metastasis and disease progression patterns that align with the tumor’s organ of origi
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Intraperitoneal/Peritoneal Dissemination Xenograft
Intraperitoneal (IP) or peritoneal dissemination xenograft models are based on the introduction of human cancer cells into the peritoneal cavity of immunodeficient mice, where they attach to peritoneal surfaces, form multicellular aggregates or spheroids, and progressively generate disseminated tumor nodules that mimic advanced peritoneal metastatic disease. These models are widely used to study ovarian cancer progression, tumor-microenvironment interactions, and intraperitoneal therapeutic responses, often incorporating bioluminescence or fluorescence imaging to longitudinally monitor tumor burden in vivo. The biological principle relies on the capacity of tumor cells such as SKOV3 or related ovarian carcinoma lines to survive in suspension, aggregate within ascites-like fluid, adhere to mesothelial surfaces, and invade peritoneal organs, thereby recapitulating human peritoneal carcinomatosis patterns observed in advanced disease.
Purity & Documentation
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Data Sheet (267 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Inhibitory Antibodies User Guide (603 KB)
References
[1]. ark JE, et al. GC1118, a novel anti-EGFR antibody, has potent KRAS mutation-independent antitumor activity compared with cetuximab in gastric cancer. Gastric Cancer. 2019 Sep;22(5):932-940. [Content Brief]
[2]. Lee K, et al. Therapeutic Efficacy of GC1118, a Novel Anti-EGFR Antibody, against Glioblastoma with High EGFR Amplification in Patient-Derived Xenografts. Cancers (Basel). 2020 Oct 31;12(11):3210. [Content Brief]
[3]. Lim Y, et al. GC1118, an Anti-EGFR Antibody with a Distinct Binding Epitope and Superior Inhibitory Activity against High-Affinity EGFR Ligands. Mol Cancer Ther. 2016 Feb;15(2):251-63. [Content Brief]
[4]. Lee HW, et al. Promising Therapeutic Efficacy of GC1118, an Anti-EGFR Antibody, against KRAS Mutation-Driven Colorectal Cancer Patient-Derived Xenografts. Int J Mol Sci. 2019 Nov 24;20(23):5894. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)