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DNA Damaging Agents

DNA Damaging Agents

Antibody-drug conjugates (ADCs) achieve precise tumor cell killing by combining cytotoxic drugs (payloads) with specific antibodies. Among various payloads, DNA-damaging agents have attracted increasing attention from research institutions and pharmaceutical companies due to their high potency, unique mechanisms of action, and promising potential in treating solid tumors. With extensive experience in chemical synthesis and professional ADC development capabilities, BOC Sciences offers end-to-end services for DNA toxin-based ADC projects—ranging from molecular design, structural optimization, linker matching, ADC conjugation, and quality analysis to CMC support—helping clients advance their research efficiently and safely.

Why Choose DNA-Damaging Payloads?

Comprehensive  Product Line

Broad-spectrum Antitumor Activity

Targets both highly proliferative and slowly proliferative tumor cells, applicable to both solid and hematologic tumors, thus expanding ADC applications.

Competitive  Pricing

Ultra-potent Cytotoxicity

Typical IC₅₀ values can reach picomolar (pM) levels; low doses can induce DNA damage, triggering cell cycle arrest and apoptosis.

Flexible  Ordering Options

Unique Mechanism of Action

Directly damages DNA through alkylation, strand breakage, or cross-linking, differing from tubulin-targeting toxins and less likely to cause drug resistance.

Strict  Quality Control Testing

Bystander Effect

Certain DNA toxins possess membrane permeability, enabling them to diffuse and kill adjacent tumor cells that do not express the target antigen, thereby improving treatment efficacy.

DNA Toxin-Based Payload Development Services

Compared with traditional payloads, DNA toxins impose greater demands on R&D capabilities due to their structural complexity, synthetic challenges, handling safety, and conjugation strategies. Backed by over 20 years of small molecule custom synthesis experience and deep expertise in antibody conjugation, BOC Sciences has established a systematic DNA toxin development platform covering the entire process from structural design and linker screening to conjugation and scale-up. We are committed to providing global clients with high-quality, efficient, and translatable custom services, accelerating early-stage validation and clinical translation of ADCs, and solving technical and process challenges during DNA payload development.

Toxin Structure Design and Synthesis Optimization

  • Development of synthetic routes for natural DNA toxin derivatives such as Calicheamicin, PBD, Duocarmycin, and Deruxtecan;
  • Design of DNA-damaging agents with specific functional groups (e.g., sulfur, amine, carboxyl) based on client targets and conjugation strategies;
  • Structural modification and derivatization to fit linkers or enhance stability/control.

Linker Design and Conjugation Strategy Development

From Lab Scale to Pilot Scale Synthesis Systems

  • Support for lab-scale synthesis (mg level) up to gram- and kilogram-level custom production;
  • Multistep organic synthesis platforms proficient in scaling up high-toxicity compounds and impurity control;
  • Experienced project management team ensures transparent processes and efficient communication.

ADC Construction and Functional Characterization

  • Complete ADC construction including antibody modification, linker conjugation, purification, and characterization;
  • Equipped with advanced instruments like LC-MS, NMR, HPLC, UV, and SEC;
  • Offers impurity analysis, metabolic stability, and batch-to-batch consistency evaluations;
  • Provides comprehensive quality reports to support clinical filings or CMO transfer.

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Service Targets and Applicable Projects

BOC Sciences provides flexible, highly customized service modules tailored to client needs at different R&D stages, supporting critical steps such as payload screening, synthesis, structural optimization, linker matching, and ADC conjugation. We deeply understand the complexity of ADC development and specialize in collaborating with clients to build efficient workflows from molecular design to functional validation, accelerating project progress, reducing R&D risks, and achieving seamless transition from concept to clinic.

Project TypeClient ScenarioRecommended Services
Lead Compound Screening Clients exploring highly active payload candidatesStructural libraries + custom screening
Payload Optimization Clients with existing structures needing solubility/stability improvementTargeted modification and derivatization
Novel ADC Design Clients with existing antibodies and targetsLinker selection + conjugation strategy support
Industrial Translation Clients preparing for IND filing or process scale-upPilot-scale process optimization + quality system support

Key Strengths in DNA Payload Development

01

Full Process Coverage

From raw material procurement, structural design, and linker development to payload conjugation, ADC construction, and quality analysis, the entire workflow is managed in-house to ensure project continuity, data traceability, and efficient delivery.

02

Professional Project Team

A dedicated team of PhDs and technical experts in organic synthesis, ADC processes, and analytical testing, with rich experience in project management and cross-functional collaboration, ensuring both scientific rigor and execution excellence.

03

Expertise in Handling Highly Active Compounds

Equipped with advanced facilities and safety systems for handling highly toxic compounds, and experienced in working with ultra-potent toxins like PBD, Calicheamicin, and Duocarmycin, ensuring safe and compliant synthesis operations.

04

Flexible Customization Services

Supports both full-process, one-stop services and stand-alone development modules (e.g., toxin design, linker screening, ADC conjugation or characterization), tailored to meet specific project needs.

05

Scalable Production Capability

Enables smooth transition from research to clinical scale, with capabilities ranging from milligram-level synthesis to gram- and kilogram-level pilot production to match various R&D stages.

06

High-Standard Quality Control System

Advanced analytical platforms including LC-MS, HPLC, and SEC, combined with a comprehensive quality control system, support systematic evaluation of key parameters such as toxin purity, conjugation efficiency, and stability.

Integrated Workflow for DNA Toxin Development

Scheme Design and Contract Customization

Toxin Structure Analysis and Strategy Formulation

Based on the mechanism of action and project characteristics, we analyze suitable DNA toxin structures (e.g., PBD, Calicheamicin), design synthetic routes, and evaluate linker compatibility and release strategies.

Payload/Linker Synthesis

Lab-Scale Synthesis and Linker Adaptation

Conduct lab-scale synthesis of small-molecule toxins, introduce functional groups, perform derivatization and linker docking experiments, and verify conjugation activity and basic stability.

Scheme Design and Contract Customization

Toxin-Payload Conjugation Optimization

Screen and optimize conjugation conditions between payload and antibody, including reaction type, solvent system, reaction time, DAR control, and purification methods.

Analysis, Purification and Characterization

ADC Construction and Purification

Complete the conjugation of antibody and payload, use chromatography or membrane separation for purification, and ensure the homogeneity, stability, and bioactivity of the ADC product.

cGMP Manufacturing and Filling

Functional Evaluation and Analytical Testing

Conduct in vitro cytotoxicity analysis, endocytosis-release studies, and plasma stability assessments. Perform DAR, purity, and structural validation using LC-MS, HPLC, SEC, and other techniques.

Result Delivery

Pilot Scale-Up and Delivery Support

Based on process feasibility verification, perform synthesis and conjugation scale-up. Support clients in transitioning from research to CMC stages, and provide batch samples with complete analytical data packages.

Frequently Asked Questions

Frequently Asked Questions

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More About DNA Damaging Agents

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