2020年1月22日 · To obtain a benchmark of A431 cell susceptibility to microtubule inhibitors (MTI), A431 monolayers were treated with either an ADC, a drug linker, or a small molecule: the forms used were the...

2021年9月3日 · S7 ADC treatment induced much higher apoptosis of A431 and MDA-MB-468 cells and triggered a substantial dose-dependent shift of tumor cell cycle from G1 phase to G2/M phase with respect to 97m ...

2018年4月1日 · The intracellular accumulation of MMAE or cys-MMAF was measured following ABBV-221 or ABT-414 incubation with A431 (A), H292 (B), and LoVo (C) cell lines. The percentage tumor uptake (%ID/cc) of 111 Indium-labeled ABT-806, AM1, or negative control human igG1 was measured by SPECT imaging in A431 …

2023年1月1日 · Only A431 cells exhibited complete killing with 40H3-MMAE, with an IC50 of less than 10 nM. Poor susceptibility to ADCs could reflect resistance to the payload being employed. To determine intrinsic drug sensitivity, each cell line was incubated with free drug.

2021年11月1日 · Cytotoxicity studies in all cell lines confirmed a high sensitivity to MMAE, with potencies of 0.24 nM to 0.81 nM (Fig. 4 B). ADC 3 demonstrated potent inhibitory activities in the MDA-MB-231, PC 9 and A431 PD-L1 + cell lines, with EC 50 values of 10.33 nM, 9.75 nM, and 11.94 nM, respectively (Fig. 4 B). In addition, we confirmed the weak ...

2023年11月1日 · Owing to its small molecular size and monovalent format, the antiEGFR Nanofitin-drug conjugate D8-vc-MMAE penetrated deeply within A431 tumor tissue, yielding to a targeting of nearly all of the tumor cells.

LR004‐VC‐MMAE showed a potent antitumor effect against ESCC and other EGFR‐positive cells with IC 50 values of nM concentrations in vitro. The in vivo antitumor effects of LR004‐VC‐MMAE were investigated in ESCC KYSE520 and A431 xenograft nude mice models.

In vivo imaging of Alexa Fluor 647-dye conjugates in A431-xenografted mice bearing subcutaneous tumors as the SCC model revealed unspecific binding of bivalent DARPins to the ubiquitously expressed EGFR. Tumor-targeting was verified 6 h …

The RC68 recognized EGFR on tumor cells, particularly for higher EGFR expressing H125, A431, HCC827 and H1975 cells. The RC68 was conjugated with an average of 4 MMAE molecules to generate RC68-MC-VC-PAB-MMAE and RC68-PY-VC-PAB-MMAE, respectively.

在初始生长阶段之后，将球状体用小分子澳瑞他汀（MMAE）或含有不可切割澳瑞他汀药物有效载荷（033-F）的抗体-药物偶联物处理。 与单层细胞相比，033-F对球体的效力明显较弱，尽管MMAE对单层和球体的效力水平相似。 更大体积的球体减少了033-F释放的有效载荷的积累，可能会导致效能差异。 尽管用033-F降低了对球体的效力，但球体体积仍很容易以剂量依赖的方式降低033-F，在所有球体尺寸的最高浓度下，球体体积均减少了> 85％。 另外，较大球体的核心显 …