Anti-ERBB2 Antibody Prodrug, Protease Activated (VS-1025-YC2)

CAT#: VS-1025-YC2

The Anti-ERBB2 Antibody Prodrug, Protease Activated (VS-1025-YC2) is an antibody prodrug comprised of a recombinant mouse antibody targeting human ErbB2, 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 ERBB2 protein. Once the masking peptide is cleaved by matrix metalloproteinases (MMPs), the prodrug is activated, allowing the unmasked monoclonal antibody component to bind to ERBB2 effectively. ErbB2, commonly known as HER2, is a receptor tyrosine kinase that acts as a major oncogenic driver when its gene is amplified or the protein is overexpressed, primarily in aggressive forms of breast and gastric cancers. Uncontrolled HER2 signaling promotes excessive cell proliferation and survival, directly contributing to tumor growth and metastasis. This makes HER2 a critical therapeutic target for which monoclonal antibodies were developed to block its activity.

Gene Expression
Figure 1 IF staining of human cell line U-251 MG Figure 2 IF staining of human cell line A-431 Figure 3 High expression in esophagus Figure 4 IHC staining of human rectum Figure 5 IHC staining of human urinary bladder Figure 6 Kidney Figure 7 Breast Figure 8 RNA cell line category: Group enriched (OE19, SK-BR-3)

Specifications

  • Host Animal
  • Mouse
  • Applications
  • In situ zymography (ISZ), Cytotoxicity assay (Cyt), Functional assay
  • Specificity
  • Human ErbB2
  • Target
  • ERBB2
  • Species Reactivity
  • Human
  • Isotype
  • IgG1, kappa
  • Masking Approach
  • Steric mask
  • Mask
  • Coiled-coiled domains
  • Purification
  • Protein G 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
  • Upon ERBB2 activation, the MEMO1-RHOA-DIAPH1 signaling pathway elicits the phosphorylation and thus the inhibition of GSK3B at cell membrane. This prevents the phosphorylation of APC and CLASP2, allowing its association with the cell membrane. In turn, membrane-bound APC allows the localization of MACF1 to the cell membrane, which is required for microtubule capture and stabilization. In the nucleus is involved in transcriptional regulation. Associates with the "5-TCAAATTC-3" sequence in the PTGS2/COX-2 promoter and activates its transcription. Implicated in transcriptional activation of CDKN1A; the function involves STAT3 and SRC.
  • Alternative Names
  • ERBB2; v-erb-b2 erythroblastic leukemia viral oncogene homolog 2, neuro/glioblastoma derived oncogene homolog (avian)
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