Anti-IGF1R (Robatumumab)-MC-Vc-PAB-DMEA-(PEG2)-duocarmycin SA ADC
Anti-IGF1R (Robatumumab)-MC-Vc-PAB-DMEA-(PEG2)-duocarmycin SA ADC (ADC-W-1255)
This ADC product is comprised of an anti-IGF1R 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.
This receptor binds insulin-like growth factor with a high affinity. It has tyrosine kinase activity. The insulin-like growth factor I receptor plays a critical role in transformation events. Cleavage of the precursor generates alpha and beta subunits. It is highly overexpressed in most malignant tissues where it functions as an anti-apoptotic agent by enhancing cell survival. Alternatively spliced transcript variants encoding distinct isoforms have been found for this gene.
ADC Antibody
Overview
Human Anti-IGF1R IgG1-kappa antibody, Robatumumab
Generic name
Robatumumab
Host animal
Human
ADC Linker
Name
MC-Vc-PAB-DMEA-(PEG2)
Description
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.