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Auristatins

Auristatins are a family of complex analogues to the native antineoplastic product dolastatin 10. They are 100 to 1000 times more toxic than Doxorubicin, a conventional cancer chemotherapy medication. https://www.creative-biolabs.com/adc/auristatins.htm

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Auristatins

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  1. Auristatins

  2. As one major component of an antibody-drug conjugate (ADC), the antibody is the key for target specificity and serves as the cargo to deliver the cytotoxic drug (payload). A payload drug can be attached to different sites on an antibody using diverse conjugation chemistry. Multiple endogenous amino acids can serve as potential conjugation sites. However, to achieve more precisely controlled site-directed conjugations and subsequently a narrower distribution of drug-to-antibody ratio (DAR), special moieties with unique conjugation chemistries are engineered into antibody sequences in our antibody design services.

  3. Antibody Design and Conjugation Some endogenous or engineered sites for the conjugation of cytotoxic payload drugs to an antibody (Antibodies,2015).

  4. To retain antibody bioactivity, mild, near-physiological conditions are often used for conjugation reactions. Under these conditions, endogenous amino acids such as Lys and Cys are chemically reactive and can be used as conjugation sites. Scientists at Creative Biolabs are experienced in performing Lysine conjugation (amine reaction) as well as Cysteine conjugation (thiol reactions) to create ADCs using these endogenous sites. We are also expertise in exploiting Tyrosine conjugation approaches as another innovated endogens site for ADC development.

  5. One downside in using the endogenous amino acids for ADC development is a heavily dispersed drug-to-antibody ratio (DAR) caused by the non-uniform distribution of the conjugation sites, especially in the case of Lysine-based conjugations.

  6. Engineered/non-engineered antibodies are conjugated to the corresponding drug-linker set designed and prepared in DrugLnk and purified via suitable liquid chromatography techniques. The resulted ADCs are characterized for some basic biochemical parameters such as DAR, stability, conjugation site distribution….

  7. Designing a chemically compatible antibody for the conjugation chemistry is a key step that directly dictates the fate of an ADC project. With expertise and dedication, advanced antibody design platform and services from Creative Biolabs will be your best companion in creating customized ADCs.

  8. About • After years of pursuit for perfection, Creative Biolabs has established our leadership in targeted immunotherapy and antibody-drug conjugate (ADC) development. Creative Biolabs offers customers with comprehensive one-stop-shop of all aspects in ADC research and evaluation, ranging from antigen selection, antibody production/optimization, payload-linker synthesis, ADC conjugation, to various stages of ADC characterization and pre-clinical evaluation. Furthermore, inventory also contains an extensive list of linkers, payloads, payload-linker sets, and commonly used ADCs for quick deployment and concept validation.

  9. Contact • 45-1 Ramsey Road, Shirley, NY 11967, USA • Email: marketing@creative-biolabs.com • www.creative-biolabs.com/car-t

  10. THANK YOU

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