This ADC product is comprised of an anti-SOST 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
- SOST; sclerostin; sclerosteosis; VBCH;
- Target Entrez Gene ID
- 50964
- Overview
- Sclerostin is a secreted glycoprotein with a C-terminal cysteine knot-like (CTCK) domain and sequence similarity to the DAN (differential screening-selected gene aberrative in neuroblastoma) family of bone morphogenetic protein (BMP) antagonists. Loss-of-function mutations in this gene are associated with an autosomal-recessive disorder, sclerosteosis, which causes progressive bone overgrowth. A deletion downstream of this gene, which causes reduced sclerostin expression, is associated with a milder form of the disorder called van Buchem disease.
ADC Antibody
- Overview
- Humanized Anti-SOST IgG4-kappa antibody, Blosozumab
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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