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. Maleimido-tri(ethylene glycol)-propionic acid also can be used as a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
性状
Liquid
IC50 & Target[1][2]
Cleavable PEGs
体外研究(In Vitro)
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 IC50 of 195 and 202 nM, respectively.ADC23 demonstrates cytotoxic activity against BT474 and N87 cell lines with IC50 of 286 and 274 nM, respectively. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Pure form -20°C 3 years;4°C 2 years
参考文献
[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.
溶解度数据
In Vitro: DMSO : 100 mg/mL (331.91 mM; Need ultrasonic)配制储备液