1. Protein Tyrosine Kinase/RTK JAK/STAT Signaling Cell Cycle/DNA Damage PI3K/Akt/mTOR
  2. EGFR PERK Akt
  3. 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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GC1118

GC1118 Chemical Structure

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Description

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[1][2][3][4].

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.

Cell Proliferation Assay[1]

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
Concentration: 0, 0.001, 0.01, 0.1, 1, 10, 100 and 1000 µg/ mL
Incubation Time: 72 h
Result: Suppressed cell growth, particularly in the MKN-45 cell line.

Cell Proliferation Assay[1]

Cell Line: SNU-484, SNU-601, SNU-719 and MKN-45 cells
Concentration: 1 µg/mL
Incubation Time: 24, 72, 120 h
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.

Western Blot Analysis[3]

Cell Line: HCT8 cells
Concentration: 0.1, 0.5, 5 and 50 μg/mL
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)
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.

Animal Model: AGS xenograft mice models (athymic nude mice, female, 6 weeks, tumor volume of 200 mm3)[1]
Dosage: 1 mg/kg
Administration: Intraperitoneally injection, twice a week for 5 weeks
Result: Showed a significant suppression of the tumor growth.
Animal Model: Patient-derived GBM xenograft models (BALB/c nude mice, female, 6-8 weeks, tumor volume of 150-200 mm3)[2]
Dosage: 50 mg/kg
Administration: Intraperitoneal injection; twice a week until euthanasia
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).
Animal Model: HCT8, Lovo, HCT15, LS174T, LS513, and SW48 xenograft mice models (athymic nude mice, 7-8 weeks, tumor volume of 200 mm3)[3]
Dosage: 1 mg/mouse
Administration: Intraperitoneally injection, twice a week for 5 weeks
Result: Significantly suppressed the tumor growth.
Animal Model: CRC-024T patient-derived xenograft mice models (BALB/c-nude mice, female, 6-8 weeks, tumor volume of 200-250 mm3)[4]
Dosage: 1 mg/mouse
Administration: Intraperitoneally injection, twice a week for 52 days
Result: Had moderate antitumor effects and no reduction in body weight.
Downregulated the levels of AKT and ERK1/2.
Gene ID

1956  [NCBI]

Accession

P00533-1

Target

EGFR

Application

ELISA, FACS, Functional assay

Conjugated

Unconjugated

Reconsititution

The product can be reconstituted/diluted with sterile PBS or saline.

SMILES

N/A

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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GC1118
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HY-P991571
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