D8-MMAD是MMAD的氘代形式。
Description | D8-MMAD is a deuterated form of MMAD, which is a microtubule disrupting agent. | ||||||||||||||||
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IC50 & Target | IC50 & Target: Tubulin[1] | ||||||||||||||||
In Vitro | 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]. | ||||||||||||||||
In Vivo | The resulting antibody-drug conjugates (ADCs) demonstrate complete tumour regression in rodents. They also have an improved toxicology profile in rats[1]. | ||||||||||||||||
Solvent & Solubility | In Vitro: DMSO : ≥ 100 mg/mL (128.35 mM) * "≥" means soluble, but saturation unknown. Preparing Stock Solutions
* Please refer to the solubility information to select the appropriate solvent. | ||||||||||||||||
References |
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