This ADC product is comprised of an anti-EPHA2 monoclonal antibody (clone 1C1)conjugated via a VC linker to a MMAE. The MMAE is targeted to certain cancers by immunerecognition and delivered into cancer cells via receptor mediated endocytosis. Within the cell, MMAE binds to tubulins, interrupts microtubule dynamics, and subsequently, induces cell death.
ADC Target
- Alternative Names
- EPHA2; EPH receptor A2; ECK; CTPA; ARCC2; CTPP1; CTRCT6; ephrin type-A receptor 2; soluble EPHA2 variant 1; tyrosine-protein kinase receptor ECK; epithelial cell receptor protein tyrosine kinase;
- Target Entrez Gene ID
- 1969
- Overview
- This gene belongs to the ephrin receptor subfamily of the protein-tyrosine kinase family. EPH and EPH-related receptors have been implicated in mediating developmental events, particularly in the nervous system. Receptors in the EPH subfamily typically have a single kinase domain and an extracellular region containing a Cys-rich domain and 2 fibronectin type III repeats. The ephrin receptors are divided into 2 groups based on the similarity of their extracellular domain sequences and their affinities for binding ephrin-A and ephrin-B ligands. This gene encodes a protein that binds ephrin-A ligands. Mutations in this gene are the cause of certain genetically-related cataract disorders.
ADC Antibody
- Overview
- Anti-EphA2 Antibody, clone # 1C1
ADC Linker
- Name
- VC (valine-citrulline)
- 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
- MMAE (Monomethyl auristatin E)
- Description
- Derived from Auristatin,are water-soluble dolastatin analogs of dolastatin 10. Dolastatin 10 belongs to dolastatin family and it can powerfully bind to tubulin, thus inhibiting polymerization mediated through the binding to the vinca alkaloid binding domain, and causes cell to accumulate in metaphase arrest.
For Research Use Only. NOT FOR CLINICAL USE.
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