- Toolbox of highly potent cytotoxic payloads with different mechanisms of action
- Design and synthesis of payload-linkers
- Guidance and advice on selection of payloads
Toolbox of Payloads
Abzena has an inventory of highly potent cytotoxic payloads with different mechanisms of action available for use in the development of ADCs. Abzena can create a range of ADCs with different payloads for screening by Abzena, customers or provide payload-linker reagents to customers undertaking their own conjugation. Abzena can also design and synthesise potent cytotoxic compounds and payloads with linkers.
Examples of payloads that Abzena can produce include:
Microtubule inhibitors stabilise or destabilise microtubules, thereby suppressing microtubule dynamics required for proper mitotic function, effectively blocking cell cycle progression and resulting in apoptosis.
- Auristatins (MMAE, MMAF, PE)
- Maytansines (DM-1, DM-4, >10 derivatives)
- Epothilone B
- Tubulysins (IM-2, B)
DNA cleavers work by the introduction of DNA strand breaks.
- Bleomycin A2
- Calicheamicin y-1
Akt is a protein kinase that plays a key role in multiple cellular processes such as apoptosis, cell proliferation, glucose metabolism, transcription and cell migration. Inhibition can lead to the induction of apoptosis.
- GDC – 0068
DNA Intercalators fit between nucleic acid base pairs preventing DNA replication
- Doxorubicin hydrochloride
- Epirubicin hydrochloride
- PBD dimers
- Oligomycin C
- Daunorubicin hydrochloride
- Topotecan and desmethyl-topotecan
DNA Transcription Inhibitors
DNA transcription inhibitors work by mechanisms such as binding transcription initiator complexes:
Cross-linking is when the agent connects two different positions either on the same strand or opposite strands of DNA. The cross-linking prevents DNA replication, leading to possible cell death and anti cancer action.
- Mitomycin C
Dihydrofolate Reductase (DHFR) Inhibitor
DHFR has a critical role in regulating the amount of tetrahydrofolate in the cell. Tetrahydofolate and its derivatives are essential for purine and thymidine synthesis, which are important for cell proliferation and cell growth.
Abzena’s team of experienced organic chemists has produced a variety of complex payloads using its custom synthesis services.
Working with Abzena
Abzena’s services are tailored for each project to ensure that the objectives are met or exceeded. Experienced project teams are assigned to each study focusing on progressing projects through to results in the minimum amount of time. Our clients widely regard us as professional and attentive partners who deliver quality results.
To get more information, a quote or to schedule a teleconference please contact us.