cetuximab

Cetuximab (C225) is a monoclonal antibody that is an inhibitor of human epidermal growth factor receptor (EGFR) (Kd=0.201 nM). Cetuximab has antitumor activity, inhibiting tumor cell proliferation and inducing apoptosis.

Cetuximab sarotalocan (Cetuximab-IRDye-700DX) is a conjugate comprising Cetuximab, an anti-EGFR monoclonal antibody, and IRdye700DX, a near-infrared photosensitizing dye. It is utilized in the study of head and neck cancers [1] [2].

Tomuzotuximab is a glycoengineered, humanized monoclonal antibody targeting the epidermal growth factor receptor (EGFR). Developed as an optimized derivative of cetuximab through glycan modification, the compound aims to enhance the clearance of EGFR-overexpressing tumor cells by boosting antibody-dependent cellular cytotoxicity (ADCC). It serves as an essential tool for investigating the synergy between receptor tyrosine kinase signaling blockade and immune effector enhancement.

Cetuximab-MMAE, an antibody-drug conjugate (ADC), combines an EGFR-targeting antibody with Monomethyl auristatin E (MMAE) to investigate colorectal and head and neck cancers.

Cetuximab (PBS) is a human IgG1 monoclonal antibody that inhibits the epidermal growth factor receptor (EGFR), with a dissociation constant (Kd) of 0.201 nM for EGFR as measured by the SPR method. It exhibits potent antitumor activity.

JBJ-07-149 is an inhibitor of EGFRL858R/T790M with an IC50 of 1.1 nM. It suppresses the proliferation of Ba/F3 cells with IC50 values of 4.9 μM when used alone, and 0.148 μM when combined with Cetuximab. Additionally, JBJ-07-149 can serve as a target protein ligand for synthesizing [DDC-01-163].

Pimurutamab (HLX-07) is a glycoengineered humanized IgG1 monoclonal antibody that specifically targets the Epidermal Growth Factor Receptor (EGFR/HER1). By binding to the extracellular domain of EGFR, Pimurutamab blocks ligand (e.g., EGF, TGF-α) binding, inhibiting receptor dimerization and downstream signaling cascades (e.g., RAS/RAF/MEK/ERK). Its optimized glycosylation profile significantly enhances Antibody-Dependent Cell-mediated Cytotoxicity (ADCC) activity. Pimurutamab is developed for treating EGFR-overexpressing solid tumors, such as colorectal cancer and head and neck squamous cell carcinoma, with potentially improved efficacy over cetuximab.

LSN3074753, a derivative of LY3009120, acts as a pan-RAF and Raf dimer inhibitor. This compound exhibits inhibitory activity against tumor cells driven by either BRAF monomers or RAF dimers, particularly in the activation of the MAPK pathway, including colorectal cancers with BRAF or KRAS mutations. When combined with Cetuximab, LSN3074753 demonstrates additive and synergistic effects in colorectal cancer PDX models, especially in those harboring KRAS or BRAF mutations.

Maleimide-PEG8-Val-Ala-PAB is an ADC linker composed of a cleavable Val-Ala-PAB linker and the probe molecule Maleimide. It is used to connect the monoclonal antibody Cetuximab with the CDK inhibitor SNS-032 for the synthesis of antibody-drug conjugates (ADC).