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Monomethyl Auristatin D

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Chemical Structure| 203849-91-6 同义名 : Demethyldolastatin 10;Monomethyl Dolastatin 10;MMAD, Demethyldolastatin 10;MMAD
CAS号 : 203849-91-6
货号 : A106511
分子式 : C41H66N6O6S
纯度 : 99%+
分子量 : 771.064
MDL号 : MFCD25976743
存储条件：

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

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 20 mg/mL(25.94 mM)，配合低频超声，并水浴加热至45℃助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
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].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.30mL

0.26mL

0.13mL

6.48mL

1.30mL

0.65mL

12.97mL

2.59mL

1.30mL
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.