|(S)-N-((3R,4S,5S)-3-甲氧基-1-((S)-2-((1R,2R)-1-甲氧基-2-甲基-3-氧代-3-(((S)-2-苯基-1-(噻唑-2-基)乙基)氨基)丙基)吡咯烷-1-基)-5-甲基-1-氧代庚-4-基)-N,3-二甲基-2-((S)-3-甲基-2-(甲基氨基)丁酰胺基)丁酰胺|CsnPharm

CAS No.: 203849-91-6

Monomethyl Auristatin D Catalog No. CSN18091

Synonyms: Demethyldolastatin 10;Monomethylauristatin D;Monomethyl Dolastatin 10

MMAD, a potent tubulin inhibitor, is a toxin payload in antibody drug conjugate.

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400-920-2911

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技术信息

生物活性

描述Microtubules (MTs)/tubulins are the largest filamentous components of the eukaryotic cytoskeleton and are essential for every cell as they control cell shape, division, motility and differentiation^[2]. MMAD (Monomethyl Dolastatin 10), a potent tubulin inhibitor, is a toxin payload in antibody-drug conjugates (ADCs) which comprise antibodies covalently attached to highly potent drugs using a variety of conjugation technologies. These conjugates were found to have good biophysical properties and a drug-to-antibody ratio (DAR) of ~1.9^[3]. The two conjugates (C16-HC-AcLys-vc-MMAD and C16-LC-AcLys-vc-MMAD) showed similar cell killing in vitro with IC₅₀ values of 0.053 and 0.054 nM, respectively, in BxPC3 pancreatic cancer cell line (M1S1 +++) and 0.058 and 0.075 nM in the A431 epidermoid carcinoma cell line (M1S1 +++). In vivo, single doses of either C16-HC-AcLys-vcMMAD (DAR 1.9) or C16-LC-AcLys-vcMMAD (DAR 1.8) at 3 mg/kg were able to induce similar tumor shrinkage percentages on week 1 and week 2 ^[4]. What's more, the resulting ADCs demonstrate complete tumour regression in rodents, which also have an improved toxicology profile in rats^[3].
临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT03465085	Acute Respiratory Distress Syn... more >>drome Severe Acute Respiratory Syndrome Collapse <<	Phase 3	Completed	-	-
NCT01889524	Normal Subjects	Not Applicable	Completed	-	Brazil ... more >> Hospital das Clínicas Recife, Pernambuco, Brazil, 50000-000 Collapse <<
NCT00306163	-	-	Completed	-	-

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参考文献

[1] Chudasama V, Maruani A, Caddick S. Recent advances in the construction of antibody-drug conjugates. Nat Chem. 2016 Feb;8(2):114-9.
[2] Gadadhar S, Bodakuntla S, Natarajan K, Janke C. The tubulin code at a glance. J Cell Sci. 2017;130(8):1347-1353.
[3] Chudasama V, Maruani A, Caddick S. Recent advances in the construction of antibody-drug conjugates [published correction appears in Nat Chem. 2016 Mar;8(3):281] [published correction appears in Nat Chem. 2016 Mar;8(3):281]. Nat Chem. 2016;8(2):114-119.
[4] Strop P, Liu SH, Dorywalska M, et al. Location matters: site of conjugation modulates stability and pharmacokinetics of antibody drug conjugates. Chem Biol. 2013;20(2):161-167.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.2969 mL
- 6.4845 mL
- 12.9691 mL
- 5 mM
- 0.2594 mL
- 1.2969 mL
- 2.5938 mL
- 10 mM
- 0.1297 mL
- 0.6485 mL
- 1.2969 mL

技术信息

CAS号

203849-91-6

储存条件

粉末: Sealed in dry,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C41H66N6O6S

运输

蓝冰

分子量

771.06

别名

Demethyldolastatin 10;Monomethylauristatin D;Monomethyl Dolastatin 10

溶解度

DMSO	115.0 mg/mL (149.1 mM)
Water	insoluble

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