MMAD(Synonyms: Demethyldolastatin 10; Monomethylauristatin D; Monomethyl Dolastatin 10)

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MMAD (Synonyms: Demethyldolastatin 10; Monomethylauristatin D; Monomethyl Dolastatin 10) 纯度: 99.86%

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。

MMAD(Synonyms: Demethyldolastatin 10; Monomethylauristatin D; Monomethyl Dolastatin 10)

MMAD Chemical Structure

CAS No. : 203849-91-6

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MMAD 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Toxins for Antibody-Drug Conjugate Research Library
  • Peptidomimetic Library

生物活性

MMAD is a potent tubulin inhibitor, is a toxin payload in antibody drug conjugates (ADCs).

IC50 & Target

Auristatin

 

体外研究
(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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

The resulting antibody-drug conjugates (ADCs) demonstrate complete tumour regression in rodents. They also have an improved toxicology profile in rats[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

771.06

Formula

C41H66N6O6S
CAS 号

203849-91-6
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

4°C, stored under nitrogen

*该产品在溶液状态不稳定，建议您现用现配，即刻使用。
溶解性数据
In Vitro: 

DMSO : 24.5 mg/mL (31.77 mM; Need ultrasonic and warming)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.2969 mL 6.4846 mL 12.9692 mL
5 mM 0.2594 mL 1.2969 mL 2.5938 mL
10 mM 0.1297 mL 0.6485 mL 1.2969 mL

*

请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液；该产品在溶液状态不稳定，建议您现用现配，即刻使用。
参考文献

  • [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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