Maleimido-tri(ethylene glycol)-propionic acid

Maleimido-tri(ethylene glycol)-propionic acid 是一种可切割的 ADC linker，用于合成抗体-药物偶联物 (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。

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100mg

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Background

Maleimido-tri(ethylene glycol)-propionic acid is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). Maleimido-tri(ethylene glycol)-propionic acid is used for the preparation of neolymphostin-based ADC precursors for site-specific cysteine mutant trastuzumab-A114C conjugation[1].

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[1].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[1].ADC24 demonstrates cytotoxic activity against BT474 and N87 cell lines with IC50 of 195 and 202 nM, respectively[1].ADC23 demonstrates cytotoxic activity against BT474 and N87 cell lines with IC50 of 286 and 274 nM, respectively[1].

[1]. Zhou D,et al. Novel PIKK inhibitor antibody-drug conjugates: Synthesis and anti-tumor activity.Bioorg Med Chem Lett. 2019 Apr 1;29(7):943-947.