MMAD-d8

D8-MMAD是MMAD的氘代形式。

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库存: 现货

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1mg

￥11875.00

9500.00

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5mg

￥26712.00

21370.00

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10mg

￥50225.00

40180.00

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货号: ajcx36340
CAS: N/A
别名: Demethyldolastatin 10-d8; Monomethylauristatin D-d8; Monomethyl Dolastatin 10-d8
分子式: C41H58D8N6O6S
分子量: 779.11
纯度: >98%
溶解度: DMSO : ≥ 100 mg/mL (128.35 mM)
储存: Store at -20°C,unstable in solution, ready to use.
库存: 现货

Background

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.