马来酰亚胺-三聚乙二醇-丙酸
| 中文名称 | 马来酰亚胺-三聚乙二醇-丙酸 |
|---|---|
| 中文同义词 | 马来酰亚胺-PEG3-酸;马来酰亚胺-三聚乙二醇-丙酸;马来酰亚胺-三聚乙二醇-羧酸;马来酰亚胺三聚乙二醇羧乙基;马来酰亚胺-三(乙烯乙二醇)-丙酸;MAI-PEG3-羧酸;3-(2-(2-(2-(2,5-二氧基-2,5-二氢-1H-吡咯-1-基)乙氧基)乙氧基)乙氧基)丙酸;3-[2-[2-[2-(2,5-二氧代-2,5-二氢-1-吡咯基)乙氧基]乙氧基]乙氧基]丙酸 |
| 英文名称 | Maleimido-Tri(Ethylene Glycol)-Propionic Acid |
| 英文同义词 | 3-(2,5-Dioxo-2,5-dihydro-1H-pyrrol-1-yl)-5-hydroxy-2,2-bis(2-hydroxyethyl)pentanoic acid;Mal-PEG3-acid;Maleimide-PEG3-CH2CH2COOH;Mal-PEG3-COOH;Maleimido-Tri(Ethylene Glycol)-Propionic Acid;Mal-PEG3-CH2CH2COOH;Propanoic acid, 3-[2-[2-[2-(2,5-dihydro-2,5-dioxo-1H-pyrrol-1-yl)ethoxy]ethoxy]ethoxy]-;3-(2,5-dioxopyrrol-1-yl)-5-hydroxy-2,2-bis(2-hydroxyethyl)pentanoic acid |
| CAS号 | 518044-40-1 |
| 分子式 | C13H19NO7 |
| 分子量 | 301.29 |
| EINECS号 | |
| 相关类别 | |
| Mol文件 | 518044-40-1.mol |
| 结构式 |  |
马来酰亚胺-三聚乙二醇-丙酸 性质
| 沸点 | 491.4±40.0 °C(Predicted) |
|---|---|
| 密度 | 1.293±0.06 g/cm3(Predicted) |
| 酸度系数(pKa) | 4.28±0.10(Predicted) |
Maleimido-tri(ethylene glycol)-propionic acid 是一种可降解 (cleavable) 的 ADC linker，用于合成抗体偶联药物 (ADCs)。Maleimido-tri(ethylene glycol)-propionic acid 用于 neolymphostin 为基础的 ADC 前体的制备，用于位点特异性半胱氨酸突变体曲妥珠单抗- A114C 的偶联。Maleimido-tri(ethylene glycol)-propionic acid 也可以用作基于 PEG 的 PROTAC Linker，可用于合成PROTAC。
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Cleavable
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PEGs
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Mal-PEG3-C2-acid can be used to synthesis linker-payload 16 (compound 15) and 20 (compound 18). linker-payload 16 amd 20 is conjugated to DAR1.9 and DAR1.7. ADC 23 and 24 are Neolymphostin ADCs that composes of DAG 1.9 and DAG1.7 linked to PIKK inhibitors with linker-payload 16 and 20, respectively. ADC24 demonstrates cytotoxic activity against BT474 and N87 cell lines with IC 50 of 195 and 202 nM, respectively. ADC23 demonstrates cytotoxic activity against BT474 and N87 cell lines with IC 50 of 286 and 274 nM, respectively.