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

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