MMAD 是一种有效的微管 (tubulin) 抑制剂,是抗体药物偶联物 (ADCs) 中的活性分子。
Description | MMAD is a potent tubulin inhibitor, is a toxin payload in antibody drug conjugates (ADCs). | ||||||||||||||||
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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 : 24.5 mg/mL (31.77 mM; Need ultrasonic and warming) Preparing Stock Solutions
* Please refer to the solubility information to select the appropriate solvent. | ||||||||||||||||
References |
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