This ADC product is comprised of an anti-PDGFR monoclonal antibody conjugated via a MC-Vc linker to 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
- PDGFRA; platelet-derived growth factor receptor, alpha polypeptide; platelet-derived growth factor receptor alpha; CD140a; PDGFR2; PDGFR-alpha; PDGF-R-alpha; CD140a antigen; PDGFRA/BCR fusion; CD140 antigen-like family member A; platelet-derived growth factor receptor 2; alpha-type platelet-derived growth factor receptor; rearranged-in-hypereosinophilia-platelet derived growth factor receptor alpha fusion protein; CD140A; PDGFR-2; RHEPDGFRA; MGC74795;
- Target Entrez Gene ID
- 5156
- Overview
- This gene encodes a cell surface tyrosine kinase receptor for members of the platelet-derived growth factor family. These growth factors are mitogens for cells of mesenchymal origin. The identity of the growth factor bound to a receptor monomer determines whether the functional receptor is a homodimer or a heterodimer, composed of both platelet-derived growth factor receptor alpha and beta polypeptides. Studies suggest that this gene plays a role in organ development, wound healing, and tumor progression. Mutations in this gene have been associated with idiopathic hypereosinophilic syndrome, somatic and familial gastrointestinal stromal tumors, and a variety of other cancers.
ADC Antibody
- Overview
- Human Anti-PDGFRA IgG1-kappa antibody, Olaratumab
ADC Linker
- Name
- MC-Vc-PAB (maleimidocaproyl-valine-citrulline-p-aminobenzoyloxycarbonyl)
- 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
- 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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