GC1118
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.
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- Pureté: 99.22%
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
Human
EGFR
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.
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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.
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.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
P00533-1
Unconjugated
The product can be reconstituted/diluted with sterile PBS or saline.
ELISA, FACS, Functional assay
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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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Livraison
Shipping with dry ice.
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Formulation
Please refer to the lot-specific COA for specific buffer information.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
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Fiche technique (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)
Références
[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)
GC1118 Related Classifications
HY-P991571 Related Classifications
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