This ADC product is comprised of an anti-CXCR4 monoclonal antibody conjugated via a MC-Vc-PAB linker to SN38. The SN-38 is targeted to certain cancers by immunerecognition and delivered into cancer cells via receptor mediated endocytosis. Within the cell, SN-38 binds to DNA, causes DNA damage.
ADC Target
- Alternative Names
- CXCR4; chemokine (C-X-C motif) receptor 4; chemokine (C X C motif), receptor 4 (fusin); C-X-C chemokine receptor type 4; CD184; D2S201E; fusin; HM89; HSY3RR; LESTR; NPY3R; NPYR; NPYY3R; CXC-R4; CXCR-4; CD184 antigen; SDF-1 receptor; neuropeptide Y receptor Y3; seven transmembrane helix receptor; stromal cell-derived factor 1 receptor; lipopolysaccharide-associated protein 3; seven-transmembrane-segment receptor, spleen; leukocyte-derived seven transmembrane domain receptor; leukocyte-derived seven-transmembrane-domain receptor; FB22; LAP3; LCR1; WHIM; NPYRL;
- Target Entrez Gene ID
- 7852
- Overview
- This gene encodes a CXC chemokine receptor specific for stromal cell-derived factor-1. The protein has 7 transmembrane regions and is located on the cell surface. It acts with the CD4 protein to support HIV entry into cells and is also highly expressed in breast cancer cells. Mutations in this gene have been associated with WHIM (warts, hypogammaglobulinemia, infections, and myelokathexis) syndrome. Alternate transcriptional splice variants, encoding different isoforms, have been characterized.
ADC Antibody
- Overview
- Human Anti-CXCR4 IgG4-kappa antibody, Ulocuplumab
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
- Name
- SN-38 (7-ethyl-10-hydroxycamptothecin)
- Description
- SN38 (7-ethyl-10-hydroxy camptothecin) is an active metabolite of the cancer prodrug, irinotecan, with the ability of inhibiting Topoisomerase I, which is belong to the camptothecin family. SN-38 is formed via hydrolysis of irinotecan by carboxylesterases and metabolized via glucuronidation by UGT1A1.
For Research Use Only. NOT FOR CLINICAL USE.
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