Duostatin
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This ADC product is composed of an anti-HER2 antibody conjugated via vc linker to Duostatin-3 (trastuzumab-vc-Duostatin-3). It has demonstrated a response in ovarian cancer treatment by a MOA (Mechanism of Action) of inhibiting cell division by blocking of tubulin polymerization.
![• Datasheet
• Specifications
• Antibody OverviewTrastuzumab
• Antibody IsotypeIgG1
• LinkerVC (valine-citrulline)
• Linker Class/DescriptionClass: Enzymatically cleavable linker-Peptide linker
• 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.
• DrugDuostatin-3
• Drug Class/DescriptionClass: Duostatin-3
• Description: Duostatin-3 is an antimitotic agent that inhibits cell division by blocking of tubulin polymerization. Unlike vcMMAE, duostatin-3 cannot kill neighboring tumor cells when the drug is released from the antibody.
• Target
• IntroductionThis gene encodes a member of the epidermal growth factor (EGF) receptor family of receptor tyrosine kinases. This protein has no ligand binding domain of its own and therefore cannot bind growth factors. However, it does bind
tightly to other ligand-bound EGF receptor family members to form a heterodimer, stabilizing ligand binding and enhancing kinase-mediated activation of downstream signalling pathways, such as those involving mitogen-activated protein
kinase and phosphatidylinositol-3 kinase. Allelic variations at amino acid positions 654 and 655 of isoform a (positions 624 and 625 of isoform b) have been reported, with the most common allele, Ile654/Ile655, shown here. Amplification and/or
overexpression of this gene has been reported in numerous cancers, including breast and ovarian tumors. Alternative splicing results in several additional transcript variants, some encoding different isoforms and others that have not been fully
characterized. [provided by RefSeq, Jul 2008]
• Alternative NamesERBB2; erb-b2 receptor tyrosine kinase 2; NEU; NGL; HER2; TKR1; CD340; HER-2
• Entrez Gene ID2064
• UniProt IDP04626](data:image/gif;base64,R0lGODlhAQABAIAAAAAAAP///yH5BAEAAAAALAAAAAABAAEAAAIBRAA7)
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Duostatin
- 1. duostatin • This ADC product is composed of an anti-HER2 antibody conjugated via vc linker to Duostatin-3 (trastuzumab-vc-Duostatin-3). It has demonstrated a response in ovarian cancer treatment by a MOA (Mechanism of Action) of inhibiting cell division by blocking of tubulin polymerization.
- 2. • Datasheet • Specifications • Antibody OverviewTrastuzumab • Antibody IsotypeIgG1 • LinkerVC (valine-citrulline) • Linker Class/DescriptionClass: Enzymatically cleavable linker-Peptide linker • 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. • DrugDuostatin-3 • Drug Class/DescriptionClass: Duostatin-3 • Description: Duostatin-3 is an antimitotic agent that inhibits cell division by blocking of tubulin polymerization. Unlike vcMMAE, duostatin-3 cannot kill neighboring tumor cells when the drug is released from the antibody. • Target • IntroductionThis gene encodes a member of the epidermal growth factor (EGF) receptor family of receptor tyrosine kinases. This protein has no ligand binding domain of its own and therefore cannot bind growth factors. However, it does bind tightly to other ligand-bound EGF receptor family members to form a heterodimer, stabilizing ligand binding and enhancing kinase-mediated activation of downstream signalling pathways, such as those involving mitogen-activated protein kinase and phosphatidylinositol-3 kinase. Allelic variations at amino acid positions 654 and 655 of isoform a (positions 624 and 625 of isoform b) have been reported, with the most common allele, Ile654/Ile655, shown here. Amplification and/or overexpression of this gene has been reported in numerous cancers, including breast and ovarian tumors. Alternative splicing results in several additional transcript variants, some encoding different isoforms and others that have not been fully characterized. [provided by RefSeq, Jul 2008] • Alternative NamesERBB2; erb-b2 receptor tyrosine kinase 2; NEU; NGL; HER2; TKR1; CD340; HER-2 • Entrez Gene ID2064 • UniProt IDP04626