MMAD-d8 (Synonyms: Demethyldolastatin 10-d8; Monomethylauristatin D-d8; Monomethyl Dolastatin 10-d8) |
| Catalog No.GC63775 |
Le D8-MMAD est une forme deutérée du MMAD, qui est un agent perturbateur des microtubules.
Products are for research use only. Not for human use. We do not sell to patients.
Sample solution is provided at 25 µL, 10mM.
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D8-MMAD is a deuterated form of MMAD, which is a microtubule disrupting agent.
MMAD (Monomethyl Dolastatin 10) is coupled through a stable oxime-ligation process to yield several near-homogenous antibody-drug conjugates (ADCs) with a drug-to-antibody ratio of ~2.0. The resulting conjugates demonstrate good pharmacokinetic properties, potent in vitro cytotoxic activity against HER2+ cancer cells. When compared with ADCs prepared by cysteine alkylation following native interchain disulfide reduction, site-specific unnatural-amino-acid-based ADCs are shown to have increased in vitro cytotoxicity[1].
The resulting antibody-drug conjugates (ADCs) demonstrate complete tumour regression in rodents. They also have an improved toxicology profile in rats[1].
[1]. Chudasama V, et al. Recent advances in the construction of antibody-drug conjugates. Nat Chem. 2016 Feb;8(2):114-9.
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