2023年6月28日 · 与微管抑制剂中观察到的纳摩尔ic50（半数最大抑制浓度）范围相比，dna损伤剂的ic50值能够达到皮摩尔水平，因此与dna损伤剂结合的adc有时更有效，并且可能独立于细胞周期（与主要作用于有丝分裂期的微管蛋白抑制剂相比），它们甚至可能用于那些抗原表达低 ...

2015年9月15日 · The half maximal inhibitory concentration (IC50 ) of MMAE was approximately 1 nM for all of the cell lines used. Meanwhile, the IC50 of anti-human ADC was 1.15 nM in the cell lines showing high TF expression, while exceeding …

MMAE, a microtubule inhibitor, the IC 50 values range from 0.23 to 1.16 nM for several cancer cell lines (33, 34). DXd, a DNA topoisomerase I inhibitor, is cytotoxic to human cancer cell lines...

2023年11月9日 · 缔码生物开发了适合ADC ELISA 测定的anti-MMAE抗体，它可用于定量测定测试样品中anti-MMAE-缀合物的水平， 可用于PK检测以及DAR值分析，加速ADC药物的研发进程。

Aurisatin E通过抑制癌细胞微管聚合，阻碍有丝分裂 [5]，对几乎所有的细胞系均具有广泛的抗增殖效果（平均IC50 = 3.2 ± 0.51 nM, 暴露1 h） [6]，效果远优于同为抗有丝分裂剂的vinblastine和doxorubicin [6]。 为方便将AE引入ADC中，其C端的二甲氨基改为甲氨基，即MMAE，可方便地与PABC间隔子进行化学连接，构成vcMMAE的连接子-载荷组合（图2）。 vcMMAE的临床效果及应用.

2020年1月22日 · The MMAE GR50 values were nearly identical, with a spheroid GR50 of 320 pM MMAE and monolayer GR50 of 291 pM MMAE. Conversely, calculated GR50 and IC50 values for 033-F treated spheroids...

PNU-159682是奈莫柔比星（Nemorubicin）的肝脏代谢物，可抑制DNA拓扑异构酶II，其效力比奈莫柔比星高三个数量级，IC50为20–100 pM，同时PNU-159682也不是外排转运蛋白的底物[5d]。

Strikingly, we found that the strong responders to the ADC in vivo also had high MMAE sensitivity in in vitro cell viability assays (IC 50 <1 nM) ( Table 2). In contrast, the moderate in vivo...

It is known that MMAE is released from the ADC following binding, internalisation and proteolytic degradation in target tissues. A striking discrepancy in systemic MMAE levels has been observed across species with 50-fold higher MMAE levels in human than that in rodents when normalised by ADC dose with unknown mechanism.

2022年7月5日 · In this work, we report a trimodal precision cytotoxic chemo-radio-immunotherapy paradigm using spatially targeted auristatin warheads. Tumor-directed antibodies and peptides conjugated to...