Anti-ERBB3 Antibody Prodrug, Protease Activated (clone 1153)

CAT#: VS-1025-YC46

The Anti-ERBB3 Antibody Prodrug, Protease Activated (clone 1153) is an antibody prodrug comprised of a recombinant mouse antibody targeting human ERBB3, linked to a masking peptide that conceals the active antigen-binding site via a protease-cleavable linker. The mask peptide is recombinantly attached to the amino terminus of either the light or heavy chain of the antibody, designed to block access to the antigen-binding site and physically prevent the antibody from binding to ERBB3 protein. Once the masking peptide is cleaved by matrix metalloproteinases (MMPs), the prodrug is activated, allowing the unmasked monoclonal antibody component to bind to ERBB3 effectively. ERBB3 (HER3) is a receptor tyrosine kinase often overexpressed in many cancers, yet it possesses little to no intrinsic kinase activity. It acts as a critical signaling platform by preferentially heterodimerizing with active HER2 or EGFR, significantly amplifying their downstream oncogenic signals, particularly the highly pro-survival PI3K/AKT pathway. This essential partnership makes HER3 a central mechanism of therapeutic resistance to anti-HER2 and anti-EGFR drugs.

Gene Expression
Figure 1 IF staining of human cell line U-2 OS Figure 2 IHC staining of human testis Figure 3 IHC staining of human small intestine Figure 4 IHC staining of human kidney Figure 5 IF staining of human cell line A-431 Figure 6 IF staining of human cell line U-251 MG Figure 7 Cerebral cortex Figure 8 Colon Figure 9 Liver Figure 10 Kidney Figure 11 Testis Figure 12 Skin Figure 13 Lymph node Figure 14 RNA cell line category: Cell line enhanced (Hep G2, OE19, RT4, SK-BR-3, SK-MEL-30, T-47d, WM-115)

Specifications

  • Host Animal
  • Mouse
  • Applications
  • In situ zymography (ISZ), Cytotoxicity assay (Cyt), Functional assay
  • Specificity
  • Human ERBB3
  • Target
  • ERBB3
  • Species Reactivity
  • Human
  • Isotype
  • IgG
  • Clone
  • clone 1153
  • Epitope
  • ERBB3-ECD
  • Masking Approach
  • Affinity mask
  • Mask
  • A synthetic peptide
  • Protease Cleavable Linker
  • MMP-cleavable linker
  • Protease Substrate
  • MMPs
  • Purification
  • Protein A purified
  • Buffer
  • PBS, pH 7.4
  • Preservative
  • No preservatives
  • Storage
  • Store at 4°C short term. For long term storage, store at -20°C, avoiding freeze/thaw cycles.

Target

  • Introduction
  • This gene encodes a member of the epidermal growth factor receptor (EGFR) family of receptor tyrosine kinases. This membrane-bound protein has a neuregulin binding domain but not an active kinase domain. It therefore can bind this ligand but not convey the signal into the cell through protein phosphorylation. However, it does form heterodimers with other EGF receptor family members which do have kinase activity. Heterodimerization leads to the activation of pathways which lead to cell proliferation or differentiation. Amplification of this gene and/or overexpression of its protein have been reported in numerous cancers, including prostate, bladder, and breast tumors. Alternate transcriptional splice variants encoding different isoforms have been characterized. One isoform lacks the intermembrane region and is secreted outside the cell. This form acts to modulate the activity of the membrane-bound form. Additional splice variants have also been reported, but they have not been thoroughly characterized.
  • Alternative Names
  • Erb-B2 Receptor Tyrosine Kinase 3; V-Erb-B2 Avian Erythroblastic Leukemia Viral Oncogene Homolog 3; Tyrosine Kinase-Type Cell Surface Receptor HER3; Human Epidermal Growth Factor Receptor 3; Proto-Oncogene-Like Protein C-ErbB-3; EC 2.7.10.1; HER3; Lethal Congenital Contracture Syndrome 2; P180-ErbB3; P45-SErbB3; P85-SErbB3; EC 2.7.10; MDA-BF-1; C-ErbB-3; C-ErbB3; ErbB3-S; ErbB-3; LCCS2
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