GC1118 (GC-1118A) is a fully human anti-EGFR monoclonal antibody with a KD value of 0.16 nM against EGFR. It potently inhibits signal transduction triggered by both high-affinity and low-affinity EGFR ligands. GC1118 exhibits strong antiproliferative activity in both KRAS wild-type and KRAS mutant cells. It can penetrate the blood-brain barrier (BBB) and blood-tumor barrier (BTB) to reach tumor sites and demonstrates excellent antitumor effects in various mouse xenograft models. GC1118 is applicable for cancer studies, including colorectal cancer.

GC1118 (GC-1118A) exhibits significant antiproliferative activity in both KRAS wild-type and KRAS mutant cells when used at 1 μg/mL for 24-120 hours. At a concentration of 100 µM over 6 days, GC1118 inhibits the growth of primary tumor cells G096 and G022. Additionally, GC1118 at concentrations ranging from 0.1-50 μg/mL for 2 hours can block both high-affinity and low-affinity ligand-induced EGFR signaling in HCT8 cells. Furthermore, the compound inhibits cell proliferation induced by both affinity types of ligands within 3 days in HCT8 cells at concentrations from 0.005-100 μg/mL.

GC1118 (GC-1118A) administered intraperitoneally at 1 mg/kg twice weekly for five weeks significantly inhibits tumor growth in AGS xenograft mouse models. At 50 mg/kg, given intraperitoneally twice weekly, GC1118 demonstrates remarkable anti-tumor activity in patient-derived GBM xenograft models. Furthermore, GC1118, at a dose of 1 mg/mouse administered intraperitoneally twice weekly for five weeks, significantly suppresses tumor growth in HCT8, Lovo, HCT15, LS174T, LS513, and SW48 xenograft mouse models. When administered at 1 mg/mouse intraperitoneally twice weekly for 52 days, GC1118 exhibits moderate anti-tumor effects in patient-derived CRC-024T xenograft mouse models.