Chemical Payloads

Chemical Payloads

BOC Sciences develops a wide variety of payloads, each with its own characteristics. Depending on the mechanism of action, chemical payloads can be divided into: anti-mitosis, DNA disruption, transcriptional inhibitors, and the like. Most of the compounds currently in clinical trials use maytansine derivatives (DM1/DM4) or auristatin (MMAE/MMAF), which are all microtubule inhibitors. These usually induce apoptosis in cells undergoing mitosis by arresting the cell cycle at G2/M. Recent studies have shown that microtubule inhibitors may also disrupt interphase non-dividing cells.

Other types of cytotoxins used in ADCs include enediynes (Calicheamicin), duocarmycin derivatives, pyrrolobenzodiazepines (PBDs), and indolinobenzodiazepines, all of which target the minor groove of DNA and the quinoline alkaloid that inhibits topoisomerase. For example, effective cytotoxic drugs that can interact doxorubicin and doxorubicin and daunorubicin by inserting DNA.

ADC chemical payloads

The payloads that BOC Sciences can produce include

  • Microtubule inhibitors

The combination of microtubule inhibitor and tubulin promotes or inhibits the assembly of microtubules, interferes with the normal structure and function of microtubules, and has the effect of interfering with cell mitosis and inhibiting cell proliferation, and exerts a clear anti-tumor effect.

  • Paclitaxel
  • Dolastatin-10
  • Auristatins (MMAE, MMAF, PE)
  • Vinorelbine
  • Epothilone B
  • Maytan (DM-1, DM-4, >10 derivatives)
  • MMAF (Monomethylauristatin F)
  • Akt Inhibitors

Akt is a protein kinase that plays an important role in cell survival and apoptosis. It also plays a key role in a variety of cellular processes, such as glucose metabolism, transcription and cell migration. Inhibition of Akt activity promotes apoptosis.

  • GDC-0068
  • Perifosine (KRX-0401)
  • Triciribine
  • DNA Intercalators

DNA intercalating agents are compounds that can be inserted into adjacent pairs of bases in a DNA duplex to bind to DNA.

  • Doxorubicin hydrochloride
  • Epirubicin hydrochloride
  • PNU-159682
  • Duocarmycins

The Chemical Payloads services that BOC Sciences can provide include

  • A series of highly effective cytotoxic payloads
  • Design payloads with different action mechanisms
  • Design and synthesis of chemical payload-linkers
  • Guidance and suggestions on the selection of chemical payloads

Our advantages

  • True loyalty and partnership
  • Skilled chemistry team
  • Fully equipped analytical support
  • High quality, low cost products
  • Advanced technology and methods
  • Comprehensive analysis of biopharmaceutical services

BOC Sciences's services are tailored to each project to ensure that goals are met or exceeded. The experienced project team is able to provide chemical payloads based on customer needs and to provide customers with payload linkers.

References:

  1. Rago, B.et al. Quantitative conjugated payload measurement using enzymatic release of antibody–drug conjugate with cleavable linker. Bioconjugate Chemistry. 2017; 28(2):620-626.
  2. Mccombs, J. R. & Owen, S. C. Antibody drug conjugates: design and selection of linker, payload and conjugation chemistry. The AAPS Journal. 2015; 17(2):339-351.
* Only for research. Not suitable for any diagnostic or therapeutic use.

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