Cleavable Linkers

CD Bioparticles has an advanced and customizable drug delivery platform to help you solve all the problems of drug delivery in one stop. We provide high-quality cleavable linkers for carrier and drug conjugation, which can help you solve:

Figure 1. Cleavable linkers. (Tsuchikama K, et al.; 2018)

The challenges you might meet:

• The drug delivery system cannot control release, has strong off-target effects, and has poor therapeutic effects.
• Contains drugs that are susceptible to degradation when exposed to blood or the surrounding environment
• Drugs can cause side effects as they are distributed throughout the body
• The contained drug has limited solubility, making formulating it for intravenous administration challenging
• Drugs have shorter circulation time
• In combination therapy, drugs need to be released sequentially or coordinatedly at the target site
• Drugs developed are susceptible to drug resistance

Cleavable Linkers Key features:

• PC Cleavable Linkers
  
  • PC Alkyne-PEG4-NHS carbonate ester
  • PC Azido-PEG11-NHS carbonate ester
  • PC Biotin-PEG3-alkyne
  • PC Biotin-PEG3-azide
  • PC Biotin-PEG3-NHS carbonate ester
  • PC DBCO-PEG3-biotin
  • PC Mal-NHS carbonate ester
  • PC Methyltetrazine-PEG4-NHS carbonate ester
  • PC SPDP-NHS carbonate ester
  • PC-Biotin-PEG4-NHS carbonate
  • PC-Biotin-PEG4-PEG3-azide
  • PC-Biotin-PEG4-PEG4-alkyne
• Dde Cleavable Linkers
  
  • Dde Biotin-PEG4-alkyne
  • Dde Biotin-PEG4-azide
  • Dde Biotin-PEG4-DBCO
  • Dde Biotin-PEG4-Picolyl azide
• β-Glucuronide Linkers
  
  • (2S,3S,4S,5R,6S)-methyl-6-(2-(3-((Fmoc-amino) propanamido)-4-PNP-3,4,5-triacetoxy-tetrahydro-2H-pyran-2-carboxylate
  • 4-Formyl-2-nitrophenyl-β-D-Glucopyranosiduronic Acid Methyl Ester 2,3,4-Triacetate
  • β-D-Glucopyranosiduronic acid, 2-amino-4-(hydroxymethyl)phenyl, methyl ester, 2,3,4-triacetate
  • β-D-tetraacetylgalactopyranoside-PEG2-azide
  • β-D-triacetylglucopyranosiduronyl methyl ester-phenol-β-Alanine
  • β-tetraacetylglucopyranoside-glycerol
  • β-tetraacetylglucopyranoside-glycol
• -S-S- Cleavable Linkers
  
  • 2-hydroxyethyl disulfide mono-Tosylate
  • Acid-PEG2-SS-PEG2-acid
  • Acid-PEG3-SS-PEG3-acid
  • Acid-PEG4-S-S-PEG4-acid
  • Acid-PEG6-SS-PEG6-acid
  • Amino-SS-PEG12-acid
  • Aminoethyl-SS-ethylalcohol
  • Aminoethyl-SS-ethylamine
  • Aminoethyl-SS-propionic acid
  • Azido-PEG3-SS-PEG3-azide
  • Azido-SS-PEG2-acid
  • Azidoethyl-PEG2-t-Butyl ester
  • Azidoethyl-SS-ethylalcohol
  • Azidoethyl-SS-ethylamine
  • Azidoethyl-SS-ethylazide
  • Azidoethyl-SS-propionic acid
  • Azidoethyl-SS-propionic NHS ester
  • Biotin-bisamido-SS-NHS
  • Bis-Tos-(2-hydroxyethyl disulfide)
  • Boc-aminooxy-ethyl-SS-propanol
  • Boc-NH-ethyl-SS-propionic acid
  • Fmoc-NH-ethyl-SS-propionic acid
  • Fmoc-NH-ethyl-SS-propionic NHS ester
  • Hydroxy-PEG3-SS-PEG3-alcohol
  • m-PEG6-SS-PEG6-methyl
  • Mal-NH-ethyl-SS-propionic acid
  • NThiol-SS-biotin
  • Propargyl-PEG1-SS-alcohol
  • Propargyl-PEG1-SS-PEG1-acid
  • Propargyl-PEG1-SS-PEG1-PFP ester
  • Propargyl-PEG1-SS-PEG1-propargyl
  • Propargyl-PEG1-SS-PEG1-t-butyl ester
  • Sulfo-NThiol-SS-biotin
  • t-Boc-Cystamine
  • THP-SS-alcohol
  • THP-SS-PEG1-t-butyl ester
  • THP-SS-PEG1-Tos
• Cleavable Peptide Linkers
• Diazo Biotin Cleavable Linkers
  
  • Diazo Biotin-PEG3-alkyne
  • Diazo Biotin-PEG3-azide
  • Diazo Biotin-PEG3-DBCO

Cleavable Linkers Key benefits:

• Low immunogenicity
• Intracellular drug release rate is higher
• Interact with or to manipulate the biological target
• Rupture resistance and specific cracking conditions
• The structure does not affect the activity of other proteases
• High tumor affinity and specificity
• Increase the hydrophilicity of the loaded drugs
• High bioavailability and biocompatibility
• Mild cracking conditions
• Suitable for in vitro and in vivo experiments
• Ready-to-use

Cleavable Linkers Application candidates:

• As an on-off switch for the release of antitumor drugs
• As a crosslinking agent to improve the stability of nanoparticles
• As a linking agent to construct nano-drug carrier
• As transfection vectors to deliver DNA and siRNA
• Construction and application of peptide/protein-conjugated drugs
• Tags for MS analysis or purification
• Study on metabolism of glucuronidation and drug metabolism in vivo
• Investigate the role of linker chemistry in enhancing drug efficacy, increasing cycle time and reducing toxicity
• Fluorescent probes for diagnostic tools, proteomic analysis or cell imaging
• Protein–protein interactions
• Activity-based protein profiling
• Elucidation of drug targets and their binding sites
• Study on covalent metabolite interactions

Reference

1. Tsuchikama K, An Z. Antibody-drug conjugates: recent advances in conjugation and linker chemistries. Protein Cell. 2018, 9(1):33-46.