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Background: EGFR (epidermal growth factor receptor), also known as ERBB-1 and HER1, is the cell-surface tyrosine kinase receptor for members of the epidermal growth factor family. Its ligands include EGF, TGFα (transforming growth factor alpha), HB-EGF (heparin-binding EGF), betacellulin, amphiregulin, epiregulin and epigen. EGFR exists as an inactive monomer until it gets activated. Upon ligand binding it forms an asymmetric dimer, for instance with HER2 (human epidermal growth factor receptor 2), which induces autophosphorylation, creating binding sites for adaptor proteins such as GRB2 (growth factor receptor-bound protein 2) and/or CBL (Casitas B-lineage lymphoma). EGFR can bind to several adaptor proteins simultaneously and thus activate multiple positive and negative signaling pathways. Overexpression and/or hyperactivation of EGFR kinase is associated with several human cancers such as lung, glioblastoma (GBM), and epithelial tumors of the neck and head, being the most common mutation in GBM and breast cancer. Mutations in EGFR can result in constantly activated EGFR, allowing tumor cell proliferation and development of resistance to drugs. Its role in cancer has led to the development of anticancer therapeutics targeting EGFR. There are several clinically approved inhibitors, such as Erlotinib and Gefitinib, for the treatment of NSCLC (non-small cell lung cancer) and pancreatic cancer. In addition, several monoclonal antibodies have also been approved, namely Cetuximab. Patients that respond to treatment to anti-EGFR therapy tend to develop resistance later on, highlighting the need for further detailed studies into the role of this protein and new therapeutic avenues.
Description: Depatuxizumab MMAE is an antibody-drug conjugate (ADC) comprising an anti EGFR monoclonal antibody (Depatuxizumab) and the cytotoxic agent Monomethyl auristatin E (MMAE). Depatuxizumab inhibits the growth of xenograft models of mutant EGFRvIII and wild-type EGFR1.
Format: Aqueous buffer solution.
Purity: ≥90%
Storage Stability: Store at -80°C, protect from light.
Target: EGFR
Uniprot: P00533
Warnings: Avoid freeze/thaw cycles.
Biosafety Level: Not applicable (BSL-1)
References: 1. Reilly EB, et al., 2015 Mol Cancer Ther. 14(5):1141-51.
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