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  5. Anti-CCR5 (PRO 140)-SMCC-DM1 ADC

Anti-CCR5 (PRO 140)-SMCC-DM1 ADC (CAT#: ADC-W-764)

This ADC product is comprised of an anti-CCR5 monoclonal antibody conjugated via a SMCC linker to DM1. The DM1 is targeted to certain cancers by immunerecognition and delivered into cancer cells via receptor mediated endocytosis. Within the cell, DM1 binds to tubulins, interrupts microtubule dynamics, and subsequently, induces cell death.

  • ADC Target
  • ADC Antibody
  • ADC Linker
  • ADC payload drug
  • Name
  • CCR5
  • Alternative Names
  • CCR5; chemokine (C-C motif) receptor 5 (gene/pseudogene); chemokine (C C motif) receptor 5 , CMKBR5; C-C chemokine receptor type 5; CC CKR 5; CD195; CKR 5; CKR5; IDDM22; chemr13; HIV-1 fusion coreceptor; chemokine receptor CCR5; C-C motif chemokine receptor 5 A159A; CCR-5; CKR-5; CCCKR5; CMKBR5; CC-CKR-5; FLJ78003;
  • Target Entrez Gene ID
  • 1234
  • Overview
  • This gene encodes a member of the beta chemokine receptor family, which is predicted to be a seven transmembrane protein similar to G protein-coupled receptors. This protein is expressed by T cells and macrophages, and is known to be an important co-receptor for macrophage-tropic virus, including HIV, to enter host cells. Defective alleles of this gene have been associated with the HIV infection resistance. The ligands of this receptor include monocyte chemoattractant protein 2 (MCP-2), macrophage inflammatory protein 1 alpha (MIP-1 alpha), macrophage inflammatory protein 1 beta (MIP-1 beta) and regulated on activation normal T expressed and secreted protein (RANTES). Expression of this gene was also detected in a promyeloblastic cell line, suggesting that this protein may play a role in granulocyte lineage proliferation and differentiation. This gene is located at the chemokine receptor gene cluster region. An allelic polymorphism in this gene results in both functional and non-functional alleles; the reference genome represents the functional allele. Two transcript variants encoding the same protein have been found for this gene.
  • Overview
  • Humanized Anti-CCR5 IgG4 antibody, PRO 140
  • Generic name
  • PRO 140
  • Host animal
  • Mouse
  • Species Reactivity
  • Human
  • Name
  • SMCC (N-succinimidyl 4-(Nmaleimidomethyl)cyclohexane-1-carboxylate)
  • Description
  • Disulfide Linkers, are extensively exploited as a chemically labile linkage. Since the release of disulfide-linked drugs requires a cytoplasmic thiol cofactor, such as glutathione (GSH). Disulfides maintain stable at physiological pH and only when ADCs are internalized inside cells, the cytosol provides reducing environment including intracellular enzyme protein disulfide isomerase, or similar enzymes, drugs can be released.
  • Name
  • DM1 (N2'-Deacetyl-N2'-(3-mercapto-1-oxopropyl)maytansine)
  • Description
  • Derived from Maytansinoid,a group of cytotoxins structurally similar to rifamycin, geldanamycin, and ansatrienin. The eponymous natural cytotoxic agent maytansine is a 19-member lactam (ansa macrolide) structure originally isolated from the Ethiopian shrub Maytenus ovatus. Maytansinoids can bind to tubulin at or near the vinblastine-binding site, which interfere the formation of microtubules and depolymerize already formed microtubules, inducing mitotic arrest in the intoxicated cells.

For Research Use Only. NOT FOR CLINICAL USE.

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