Anti-EGFR (Nimotuzumab)-MC-Vc-PAB-DMEA-(PEG2)-duocarmycin SA ADC
Anti-EGFR (Nimotuzumab)-MC-Vc-PAB-DMEA-(PEG2)-duocarmycin SA ADC (ADC-W-1063)
This ADC product is comprised of an anti-EGFR monoclonal antibody conjugated via a MC-Vc-PAB-DMEA-(PEG2) linker to duocarmycin SA. The duocarmycin SA is targeted to certain cancers by immunerecognition and delivered into cancer cells via receptor mediated endocytosis. Within the cell, duocarmycin SA binds to DNA, causes DNA damage.
ADC Target
Name
EGFR
Alternative Names
EGFR; epidermal growth factor receptor; epidermal growth factor receptor (avian erythroblastic leukemia viral (v erb b) oncogene homolog) , ERBB; ERBB1; erythroblastic leukemia viral (v erb b) oncogene homolog (avian); proto-oncogene c-ErbB-1; cell growthcur after internalization of the ADC via antigen-mediated endocytosis and delivery to lysosomal compartment, where the antibody is degraded to the level of amino acids through intracellular pro
The protein encoded by this gene is a transmembrane glycoprotein that is a member of the protein kinase superfamily. This protein is a receptor for members of the epidermal growth factor family. EGFR is a cell surface protein that binds to epidermal growth factor. Binding of the protein to a ligand induces receptor dimerization and tyrosine autophosphorylation and leads to cell proliferation. Mutations in this gene are associated with lung cancer. Multiple alternatively spliced transcript variants that encode different protein isoforms have been found for this gene.
Peptide linkers, belonging to Enzymatically cleavable linkers, combine greater systemic stability with rapid enzymatic release of the drug in the target cell. The scission of peptidic bonds relies on lysosomal proteolytic enzymes, which have very low activities in blood due to endogenous inhibitors and the unfavorably high pH value of blood.
ADC payload drug
Name
duocarmycin SA
Description
Duocarmycins SA belong to the minor-groove-binding DNA-alkylating agents (DNA MGBA). The natural duocarmycins are isolated from the culture broth of Streptmyces sp and a series of derivatives has also been synthesized.