Anti-ESR1 Antibody Prodrug, Protease Activated (VS-1025-YC49)

CAT#: VS-1025-YC49

The Anti-ESR1 Antibody Prodrug, Protease Activated (VS-1025-YC49) is an antibody prodrug comprised of a recombinant human antibody targeting human ESR1, 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 ESR1 protein. Once the masking peptide is cleaved by matrix metalloproteinases (MMPs), the prodrug is activated, allowing the unmasked monoclonal antibody component to bind to ESR1 effectively. ESR1 (Estrogen Receptor 1) is a nuclear receptor whose presence defines most hormone-sensitive breast cancers, where it acts as a transcriptional factor driven by estrogen. The resulting proliferation of the tumor cells is the basis for endocrine therapy. Furthermore, acquired mutations in ESR1 are a common mechanism of resistance to these therapies in metastatic disease.

Gene Expression
Figure 1 IF staining of human cell line MCF7 Figure 2 IF staining of human cell line RT4 Figure 3 IF staining of human cell line U-2 OS Figure 4 Endometrium Figure 5 RNA cell line category: Group enriched (MCF7, T-47d)

Specifications

  • Host Animal
  • Human
  • Applications
  • In situ zymography (ISZ), Cytotoxicity assay (Cyt), Functional assay
  • Specificity
  • Human ESR1
  • Target
  • ESR1
  • Species Reactivity
  • Human
  • 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 is an antibody binds to ER-α36, ER-α36 positively regulates HER2 expression and the population of ALDH1 positive breast cancer cells, and suggested that non-genomic estrogen signaling mediated by ER-α36 is involved in maintenance and regulation of breast cancer stem cells.
  • Alternative Names
  • ESR1; estrogen receptor 1
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