15 Jun [MCE] Isotope-Labeled ADC Cytotoxin-Assist in the new ADC drugs development
Antibody-drug conjugates (ADCs) are targeted drugs composed of antibodies, linkers and cytotoxic molecules. Unlike chemotherapy, ADCs target and kill tumor cells without harming healthy cells, by integrating the antigen specificity of monoclonal antibodies (mAbs) with antibody fragments. The ADC cytotoxin (also known as the payload) is the most important component, as it determines the potency of the ADCs to kill cancer cells. It is the “bullet” responsible for destroying cancer cells. Most of the currently developed ADCs are used to treat hematological malignancies and solid tumors, but the use of ADCs to treat autoimmune diseases, metabolic diseases has enormous potential.
ADC
Currently, there are two types of ADC cytotoxins commonly used: microtubule inhibitor drugs (such as MMAE) and DNA-damaging drugs (such as Exatecan). In addition, there are numbers of traditional cytotoxic agents with similar mechanisms of killing cancer cells which can also be used in the development of ADCs (such as: Paclitaxel).
The quantitative detection of ADC cytotoxins and their metabolites in the blood of ADC drugs can provide important reference data for their pharmacokinetics and biodistribution, which is one of the critical steps enabling their successful development and optimization. Isotope-labeled cytotoxin (such as MMAE-d8, Exatecan-d5 mesylate) has become the gold standard for quantitative detection due to the no matrix effects and high sensitivity in LCMS. This provides important data support for their pharmacokinetics and biodistribution, but also facilitates the development of ADC new drugs.
Isotope-labeled ADC cytotoxins structures
Due to the complex structure and various forms of ADC drugs with the characteristics of both macromolecules and small molecules, and the continuous development of mass spectrometry technology, LCMS technology can be used not only for small molecules but also for the characterization and quantification of macromolecules. It also brings convenience to the quantitative analysis of ADC drugs in biological matrices. Isotope-labeled compounds have become the gold standard for quantitative detection because of the ideal ionization efficiency and high sensitivity in LCMS detection, so isotope-labeled toxin molecules provide convenience for ADC drug development and pharmacokinetic research. MedChemExpress (MCE) can provide the most commonly used isotope-labeled toxin molecules in ADC research and development, such as MMAE-d8, Exatecan-d5 mesylate, Dxd-d5, SN-38-d3, etc. We can also provide customization according to your needs.
| Catalog_No | Name | Description |
| HY-15162A | MMAE-d8 | A deuterated labeled MMAE, a potent mitotic inhibitor and a tubulin inhibitor. |
| HY-13631AS | Exatecan-d5 mesylate |
A deuterium labeled Exatecan mesylate, Exatecan mesylate is a DNA topoisomerase I inhibitor. |
| HY-13631DS | Dxd-d5 | A deuterium labeled Dxd, Dxd is a potent DNA topoisomerase I inhibitor. |
| HY-15579AS | MMAF-d8 hydrochloride |
A deuterated form of MMAF hydrochloride, which is a microtubule disrupting agent. |
| HY-13704S | SN-38-d3 | A deuterium labeled SN-38. SN-38 (NK012) is an active metabolite of the Topoisomerase I inhibitor Irinotecan. SN-38 (NK012) inhibits DNA and RNA synthesis. |
| HY-13704S1 | SN-38-d5 | A deuterium labeled SN-38. SN-38 (NK012) is an active metabolite of the Topoisomerase I inhibitor Irinotecan. SN-38 (NK012) inhibits DNA and RNA synthesis. |
| HY-13442AS | Eribulin-d3 mesylate |
A deuterium labeled Eribulin mesylate. Eribulin mesylate is a microtubule targeting agent that is used for the research of cancer. |
| HY-16560S | Camptothecin-d5 | A deuterium labeled Camptothecin. Camptothecin (CPT), a kind of alkaloid, is a DNA topoisomerase I (Topo I) inhibitor. |
| HY-15581S | MMAD-d8 | A deuterated form of MMAD, which is a microtubule disrupting agent. |
| HY-12454S | DM4-d6 | A deuterium labeled DM4. DM4 is an antitubulin agent that inhibit cell division. |
| HY-12522S | PF-06380101-d8 | A deuterium labeled PF-06380101. PF-06380101, an Auristatin microtubule inhibitor. |
| HY-14519S | Methotrexate-d3 | A deuterium labeled Methotrexate used for the research of rheumatoid arthritis and a number of different cancers (such as acute lymphoblastic leukemia. |
| HY-B0015S | Paclitaxel-d5 | A deuterium-labeled Paclitaxel. Paclitaxel is a naturally occurring antineoplastic agent and stabilizes tubulin polymerization. |
| HY-B0015S1 | Paclitaxel-d5 benzoyloxy |
A deuterium-labeled Paclitaxel. Paclitaxel is a naturally occurring antineoplastic agent and stabilizes tubulin polymerization. |
MCE specializes in research and development of Isotope-Labeled Compounds and can provide different Isotope-Labeled ADC cytotoxins (ADC payloads) to meet your new ADC drug research. For our complete list of Isotope-Labeled Compounds, please visit us here.
https://www.medchemexpress.com/isotope-compound/isotope-compound.html
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