Necitumumab

Necitumumab (11F8; IMC-11F8; LY3012211) is a human IgG monoclonal antibody directed against EGFR. Necitumumab binds to the EGF binding site of EGFR, blocks ligand binding, neutralizes ligand-induced EGFR phosphorylation and downstream signaling, induces EGFR internalization and degradation, and mediates antibody-dependent cellular cytotoxicity (ADCC) in EGFR-expressing cells. Necitumumab enhances antitumour activity in combination with Gemcitabine (HY-17026) and Cisplatin (HY-17394) in murine non-small-cell lung cancer xenograft models. Necitumumab can be used in research on cancers such as non-small cell lung cancer and colorectal cancer^[1][2]. IC50 & Target:ERBB1/EGFR/HER1 In Vitro:Necitumumab specifically binds to the EGF binding site of human EGFR with high affinity (dissociation constant 0.32 nM) and blocks ligand binding with an IC₅₀ of 1-2 nM^[1].
Necitumumab neutralizes ligand-induced EGFR phosphorylation with an IC₅₀ of 1.5-3 nM^[1].
Necitumumab inhibits the proliferation of EGFR-dependent colorectal tumour cells with an IC₅₀ of 0.8-1.0 nM^[1].
Necitumumab induces EGFR internalization and degradation, and triggers antibody-dependent cellular cytotoxicity in EGFR-expressing human cells^[1]. In Vivo:Necitumumab (60 mg/kg; i.p.; twice a week for 2 weeks) yields substantially increased anti-tumour activity in murine non-small-cell lung cancer xenograft models when added to Gemcitabine (HY-17026) and Cisplatin (HY-17394)^[2].