Anti-CD20-CL2A-SN-38 ADC

CAT#: ADC-021LCT

This ADC product is composed of an anti-CD20 antibody conjuagated via a CL2A linker to SN-38 (CL2A-SN-38). It has demonstrated a response in CD20+ B-lymphoma treatment by a MOA (Mechanism of Action) of Inhibit Topoisomerase I and cause DNA damage.

Gene Expression
Figure 1 IF staining of human cell line REH Figure 2 IF staining of human cell line A-431 Figure 3 IF staining of human cell line U-2 OS Figure 4 Colon Figure 5 Bone marrow Figure 6 Lymph node Figure 7 RNA cell line category: Group enriched (Daudi, U-698)

Specifications

  • Antibody Overview
  • Humanized monoclonal Antibody targeting CD20
  • Antibody Isotype
  • IgG1κ
  • Linker
  • CL2A
  • Linker Class/Description
  • Class: 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.
  • Drug
  • SN-38 (7-ethyl-10-hydroxycamptothecin)
  • Drug Class/Description
  • Class: SN-38
    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

Target

  • Introduction
  • This gene encodes a member of the membrane-spanning 4A gene family. Members of this nascent protein family are characterized by common structural features and similar intron/exon splice boundaries and display unique expression patterns among hematopoietic cells and nonlymphoid tissues. This gene encodes a B-lymphocyte surface molecule which plays a role in the development and differentiation of B-cells into plasma cells. This family member is localized to 11q12, among a cluster of family members. Alternative splicing of this gene results in two transcript variants which encode the same protein. [provided by RefSeq, Jul 2008]
  • Alternative Names
  • MS4A1; membrane-spanning 4-domains, subfamily A, member 1; B1; S7; Bp35; CD20; CVID5; MS4A2; LEU-16; B-lymphocyte antigen CD20; CD20 antigen; CD20 receptor; leukocyte surface antigen Leu-16; B-lymphocyte cell-surface antigen B1;
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Breast cancer biomarkers at key points during disease progression
Novel SN-38 Payload Utility
Integrating the SN-38 payload, an active metabolite of irinotecan, into an ADC format targeting CD20 has provided interesting data for our B-lymphoma models. The inhibition of Topoisomerase I caused significant DNA damage in the target cells, offering a different mechanism of action compared to standard tubulin inhibitors.
Breast cancer biomarkers at key points during disease progression
Effective CL2A Peptide Linker
The CL2A linker used in this product is a great example of an enzymatically cleavable peptide linker. We observed rapid enzymatic release of the drug within the target cells, likely due to lysosomal proteolytic enzymes. At the same time, the systemic stability in our simulated fluid assays was commendable.

Q&As

  1. Where does the SN-38 payload originate from?

    A: SN-38 (7-ethyl-10-hydroxy camptothecin) is an active metabolite of the prodrug irinotecan. It belongs to the camptothecin family and is formed via hydrolysis of irinotecan by carboxylesterases. It functions by inhibiting Topoisomerase I and causing DNA damage.

  2. How does the CL2A linker release the drug?

    A: The CL2A linker is a peptide linker belonging to the class of enzymatically cleavable linkers. The scission of its peptidic bonds relies on lysosomal proteolytic enzymes. These enzymes have high activity inside the target cell but low activity in the blood, ensuring stability during circulation.

View the frequently asked questions answered by Creative Biolabs Support.

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