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Click Chemistry Conjugation

Click Chemistry Conjugation

With a strong foundation in synthetic chemistry and biotechnology, BOC Sciences supports end-to-end services covering antibody screening, linker design, drug payload preparation, and optimization of conjugation strategies, meeting the diverse needs at different stages of R&D. The platform is equipped with advanced analytical instruments and a production environment that meets quality standards, enabling processes from small-scale development to GMP-grade pilot and scale-up production, ensuring excellent product stability, safety, and consistency. We place particular emphasis on customized client requirements and offer modular, scalable project management with high responsiveness and scientific rigor to accelerate the development and translation of ADC projects.

Why Choose Click Chemistry for ADC Conjugation?

Comprehensive  Product Line

High Selectivity and
Biocompatibility

Click reactions are highly adaptable to solvents, aqueous environments, and temperature, making them especially suitable for the modification of biomolecules like proteins, without requiring prior protection or activation of other functional groups.

Competitive  Pricing

Controlled Drug-to-Antibody
Ratio (DAR)

Enables site-specific conjugation or control over the number of drug molecules conjugated, which is beneficial for optimizing the pharmacokinetic properties and therapeutic window of ADCs.

Flexible  Ordering Options

Diverse Reaction Types and
Linker Options

Multiple types of click reactions are available, such as copper-catalyzed azide-alkyne cycloaddition (CuAAC), strain-promoted azide-alkyne cycloaddition (SPAAC), offering high selectivity and adaptability for various ADC design requirements.

Strict  Quality Control Testing

Stability and
Safety

Click linkers are chemically stable and resistant to hydrolysis, significantly enhancing the in vivo stability and targeted drug release of ADCs.

Click Chemistry Conjugation Services by BOC Sciences

In ADC construction, click chemistry provides an ideal pathway for precise conjugation due to its high selectivity, bioorthogonality, and operational simplicity. BOC Sciences integrates click chemistry into multiple key stages of antibody-drug conjugation. By precisely controlling reaction sites, drug-to-antibody ratios, and conjugation methods, we ensure ADC uniformity and functional optimization. We develop multi-dimensional click chemistry strategies tailored to the characteristics of target molecules and clinical requirements, empowering innovation throughout the entire ADC development cycle—from early screening to clinical progression.

Site-Specific Conjugation

Enzyme-based or genetic engineering approaches are used to introduce alkyne/azide modification sites on antibodies, enabling highly precise site-specific conjugation to ensure product consistency.

Modular Construction Design

Antibodies, linkers, and toxins are modified with corresponding functional groups and "assembled" via click reactions, enabling rapid screening and high-throughput ADC construction.

Metal-Free System Optimization

SPAAC and IEDDA systems are prioritized to minimize protein contamination and reduce purification burden, enhancing biosafety.

Stability and Release Mechanism Integration

By tuning linker designs (e.g., ester bonds, disulfide bonds, self-immolative structures), we ensure in vivo stability while achieving efficient drug release in the tumor microenvironment.

Parallel Click Conjugation and DAR Control

Through controlled modification sites and reaction conditions, fixed DAR (e.g., 2, 4, 8) products are constructed to optimize the in vivo distribution and efficacy of ADCs.

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Click Chemistry Technology Platforms

BOC Sciences deeply understands the unique advantages of click chemistry in bioorthogonal reactions and has long been committed to the development and optimization of various click systems to meet the high-efficiency conjugation needs between antibodies, drug payloads, and linkers. By integrating cutting-edge technologies and extensive project experience, we have established multiple click chemistry platforms for ADC development, covering both classical and novel reaction mechanisms to ensure optimal results in conjugation efficiency, site specificity, and product purity. BOC Sciences provides customized click reaction design and implementation strategies to support the high-quality, controlled construction of ADCs, offering robust solutions for the precise crosslinking of complex drug molecules.

CuAAC Reaction

  • Reaction Principle: Alkynes and azides undergo 1,3-dipolar cycloaddition catalyzed by copper;
  • Advantages: Fast reaction rate, high selectivity, stable products;
  • Suitability: Ideal for antibodies or drugs that are not sensitive to copper; suitable for in vitro synthesis.

SPAAC Reaction

  • Reaction Principle: Strained cyclic alkynes (e.g., DIBO, DBCO) react rapidly with azides without a catalyst;
  • Advantages: No metal catalyst required, suitable for sensitive protein drug modifications;
  • Suitability: Ideal for in situ modifications and in vivo conjugation reactions.

IEDDA Reaction

  • Reaction Principle: Reaction between tetrazines and strained alkenes (e.g., TCO);
  • Advantages: Extremely fast, highly bioorthogonal;
  • Suitability: Particularly suitable for rapid conjugation between antibodies and small molecules in ADC construction.

Thiol-Ene Click Reaction

  • Reaction Principle: Thiols and alkenes undergo addition under light or heat;
  • Advantages: Mild conditions, compatible with various biomolecules;
  • Suitability: Enables efficient coupling without compromising antibody activity.

Service Capabilities and Advantages

01

Comprehensive One-Stop Services

From toxin and linker customization, antibody modification, click conjugation, analytical verification, to GMP-scale production, BOC Sciences offers a complete technical cycle from laboratory research to clinical development.

02

Extensive Click Chemistry Reagent Library

We maintain a broad inventory of functionalized reagents including alkynes (–C≡CH), azides (–N₃), and strained alkynes (e.g., DBCO, BCN), supporting the development of various click chemistry pathways.

03

Flexible Reaction Platform Configuration

Whether for small-scale screening, process development, or pilot and GMP-scale production, BOC Sciences provides a complete set of reaction platforms and supporting facilities. Our conjugation reactors enable precise and scalable implementation.

04

Site-Specific and Targeted Modification Technologies

We design personalized conjugation strategies based on client molecular structures, utilizing the orthogonality of click reaction sites to construct site-specific or dual-site ADCs, significantly enhancing product consistency and pharmacokinetic profiles.

Click Chemistry-Enabled ADC Workflow: From Design to Delivery

Scheme Design and Contract Customization

ADC Design and Consulting Services

  • Antibody screening and engineering recommendations
  • Linker design and click strategy selection (CuAAC, SPAAC, Bioorthogonal)
  • Drug payload and toxin evaluation
  • Conjugation site engineering and structural modeling

Payload/Linker Synthesis

Raw Material Customization and Synthesis

  • Synthesis of azide/alkyne drug precursors
  • Preparation of strained alkynes (e.g., DBCO) and tetrazine-modified intermediates
  • Synthesis of linkers containing clickable sites
  • Construction of multifunctional linkers (Cleavable/Non-cleavable)

Scheme Design and Contract Customization

Click Conjugation Implementation

  • Screening and optimization of efficient click reaction conditions
  • Click conjugation of antibodies and toxins (SPAAC, CuAAC)
  • Dual-drug loading and multi-site modification
  • Support for small-scale screening and kilogram-level pilot scale-up

Analysis, Purification and Characterization

Analytical Characterization and Stability Assessment

  • Conjugation efficiency and DAR determination
  • Characterization by SEC-HPLC, LC-MS, CE-SDS
  • Antigen-binding activity validation (ELISA, SPR)
  • Stability and solubility testing
  • Residual metal (Cu) analysis and clearance validation (applicable to CuAAC)

cGMP Manufacturing and Filling

Scale-Up Process Development and GMP Manufacturing

  • Development of large-scale conjugation processes
  • Supply of GLP/GMP-grade batches for preclinical and clinical studies
  • cGMP-compliant cleanroom facilities and isolation systems
  • Flexible production capacity for multiple scales and batch sizes

Result Delivery

Quality Control and Documentation Support

  • Provision of COA, analytical methods, MSDS, and regulatory compliance documents
  • Full-process traceability of material batches, sample retention, and data recording
  • Technical documentation and quality dossiers for CMC, BLA, IND, and other regulatory submissions
  • Regular third-party GMP audits and support for client quality system audits and on-site inspections

Frequently Asked Questions

Frequently Asked Questions

Still have questions?

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More About Antibody Conjugation

* Only for research. Not suitable for any diagnostic or therapeutic use.
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