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Microtubule Inhibitors

Microtubule Inhibitors

BOC Sciences is committed to providing efficient and reliable payload development services for antibody-drug conjugates (ADCs). As one of the most commonly used classes of cytotoxins in ADCs, microtubule inhibitors such as MMAE, MMAF, DM1, and DM4 are widely applied in numerous clinical and investigational ADC programs due to their excellent antitumor activity and mature conjugation characteristics. Leveraging our extensive synthesis experience, diverse structural resources, and modular linker-toxin design capabilities, we offer end-to-end services from structural customization, small-scale synthesis, and process optimization to gram- or kilogram-scale production, ensuring smooth progression through early pharmacodynamic validation and preclinical development. BOC Sciences, driven by technological innovation and rigorous quality control, empowers global ADC development teams to accelerate the creation of next-generation precision therapeutics.

Overcoming Bottlenecks in Tubulin Toxin Development

Comprehensive  Product Line

Lengthy Synthetic Pathways

Tubulin inhibitors possess complex, highly chiral structures and require stringent reaction conditions. During scale-up, issues such as impurity accumulation and yield reduction often arise. With our advanced multi-step organic synthesis platform and scale-up expertise, we optimize processes and control key steps to achieve high-purity synthesis from milligram to kilogram scales.

Competitive  Pricing

Challenging Conjugation Site Design

Introducing functional groups to tubulin toxins requires precise site-specific modification, as any deviation may compromise biological activity. We provide structural modification simulations and targeted functional group installation services to enable stable and controlled linker integration without disrupting the toxin's core structure.

Flexible  Ordering Options

High Hydrophobicity Impacts ADC Stability

The strong hydrophobicity of tubulin inhibitors can lead to ADC aggregation and precipitation, compromising drug consistency and clinical safety. BOC Sciences offers hydrophilic modifications for hydrophobic toxins, DAR optimization, and conjugation condition refinement to enhance solubility, stability, and formulation uniformity of ADCs.

Strict  Quality Control Testing

Linker Selection Must Precisely Match the Toxin

Improper linker design can impair intracellular toxin release at the target site, reducing ADC therapeutic efficacy. With extensive experience in synthesizing various linker types, we design cleavable or non-cleavable linkers tailored to specific tubulin inhibitors, ensuring efficient and targeted toxin release.

Comprehensive Microtubule Inhibitor Development Services

BOC Sciences is dedicated to delivering comprehensive, professional, and high-quality microtubule inhibitor development services for ADCs, supporting the entire process from early research to preclinical studies. We integrate advanced synthesis technologies, linker chemistry, toxin structure optimization, and a stringent quality control system to create a competitive service offering, which includes:

Diverse Microtubule Inhibitor Structural Library

We maintain a complete library of microtubule inhibitors, covering various natural, semi-synthetic, and fully synthetic cytotoxic structures, including:

  • Classic representative compounds: such as MMAE, MMAF, DM1, DM4, which are widely used in approved ADCs.
  • Strong structural modification capability: including functional group introduction, conjugation site optimization, and stereochemistry adjustment to enhance conjugation efficiency and targeted release.
  • Novel toxin discovery: leveraging structure-activity relationship (SAR) studies to develop non-traditional microtubule-targeting agents, expanding innovation and specificity in ADC toxin combinations.

Highly Adjustable Linker-Payload Customization Services

Linkers play a key role in controlling ADC pharmacodynamics. BOC Sciences provides multiple conjugation strategies and matching site designs:

End-to-End Toxin Development and Conjugation Solutions

With advanced synthesis platforms and conjugation technologies, BOC Sciences provides integrated solutions from toxin development to ADC construction, including:

Analytical and Quality Control Support

To ensure smooth project advancement, we are equipped with a comprehensive analytical platform for precise quality monitoring at every critical step.

DAR control and assessment:

  • DAR values can be controlled within the ideal range (e.g., 2–4) by adjusting toxin ratios and conjugation conditions
  • High-resolution LC-MS and UV methods are used to confirm DAR distribution

Toxin and intermediate analysis:

  • High-performance liquid chromatography (HPLC)
  • Nuclear magnetic resonance (NMR) and mass spectrometry (MS)
  • Melting point, optical rotation, and purity testing

Conjugate analysis:

  • Size exclusion chromatography (SEC-HPLC)
  • Capillary electrophoresis (CE-SDS)
  • Antigen-binding capability verification (e.g., ELISA, SPR)

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Why Choose BOC Sciences?

01

Rich Experience

BOC Sciences has years of expertise in developing ADC toxins and linkers. We have successfully supported multiple international ADC projects covering all stages from early screening to preclinical studies, with mature and reliable technical routes.

02

Structural Diversity

We offer a variety of microtubule inhibitor structures including MMAE, MMAF, DM1, DM4, and their derivatives, and support the custom development of innovative toxins with specific functional groups as needed by our clients.

03

Strong Customization Capability

We provide services such as toxin structure modification, linker selection optimization, and linker-toxin module design to ensure structural and functional compatibility of ADCs and enhance project success rates.

04

End-to-End Quality Control

From raw materials and intermediates to final toxins and conjugates, we employ HPLC, MS, NMR, and other analytical methods to ensure product purity, activity, and batch-to-batch consistency.

05

Global Customer Base

BOC Sciences serves hundreds of biotechnology companies, pharmaceutical enterprises, and research institutions worldwide. Our projects span key markets across North America, Europe, and Asia, earning broad customer trust and long-term partnerships.

06

Flexible Delivery and Rapid Response

We support rapid project initiation, phased delivery, and small-scale trial production. Our team provides technical consultations and development recommendations to help clients advance ADC projects under tight timelines.

07

Regulatory Compliance Support

We offer products compliant with GLP/GMP standards along with complete documentation support, including CoA, analytical reports, and stability data, facilitating smooth IND or clinical submissions.

08

Integrated Service Platform

Beyond providing toxins and linkers, we offer comprehensive services including ADC conjugation, analytical method development, and biological activity validation—creating a one-stop collaboration model to enhance development efficiency.

Tubulin Inhibitor Synthesis and Scale-Up Service Workflow

Scheme Design and Contract Customization

Requirement Assessment and Project Design

At project initiation, we engage in in-depth communication with clients to clarify the desired tubulin inhibitor structure, intended use (screening, conjugation, or preclinical), purity requirements, and batch size. We then formulate a rational synthetic route, process parameters, and delivery schedule to ensure efficient downstream development.

Payload/Linker Synthesis

Toxin Structure Design and Route Optimization

Based on the target molecule, we assess existing literature and databases to design a suitable retrosynthetic pathway. We optimize key intermediates and reaction conditions to improve efficiency and yield, reduce impurities, and ensure the scalability and consistency of the process.

Scheme Design and Contract Customization

Lab-Scale Synthesis and Key Step Verification

We perform small-scale synthesis in the lab to validate the feasibility and reproducibility of each step. Structural confirmation (NMR, MS), purity analysis (HPLC), and intermediate evaluation are completed to lay a solid foundation for scale-up while identifying potential risk points for optimization.

Analysis, Purification and Characterization

Pilot-Scale Expansion and Process Release

Under guaranteed quality, reaction scale is gradually increased to gram or higher levels. Stable and efficient reaction and purification processes are used for pilot production. Process control parameters for key steps are established to ensure smooth transition from lab to plant-scale production.

cGMP Manufacturing and Filling

High-Purity Product Purification and Quality Control

Multi-step chromatographic separation, recrystallization, or membrane separation techniques are employed for in-depth purification of the target toxin, ensuring >98% purity. Comprehensive quality analyses are conducted, including structure confirmation, impurity profiling, and residual solvent detection, to ensure each batch meets delivery standards.

Result Delivery

Packaging, Storage, and Compliance Documentation Delivery

Final products are sealed with internal packaging materials and stored under light-protected/refrigerated conditions to maintain toxin stability and activity. We provide clients with detailed synthetic routes, analytical reports, Certificates of Analysis (CoA), and Safety Data Sheets (SDS) to support R&D or regulatory filing requirements.

Frequently Asked Questions

Frequently Asked Questions

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More About Microtubule Inhibitors

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