VCMMAE (mc-vc-PAB-MMAE) is a drug-linker conjugate for ADC with potent antitumor activity.

MMAE通过计划和剂量依赖的方式使结直肠癌和胰腺癌细胞对IR敏感，其机制与有丝分裂阻滞相关。Monomethyl auristatin E (MMAE) 在CD30+癌细胞内从SGN-35中高效释放，并由于其膜透性，具备对旁观者细胞施加细胞毒活性的能力。辐射增敏作用通过减少辐照细胞的克隆存活率和增加DNA双链断裂得以证实。

Monomethyl auristatin E (MMAE) 与 IR 结合使用，能增强 DNA 损伤信号传导和 CHK1 激活，从而延缓肿瘤生长。针对肿瘤的 ACPP-cRGD-MMAE 与 IR 共同作用，在异种移植模型中产生了更为显著且持久的肿瘤退缩效果。

Monomethyl auristatin E is reconstituted in DMSO at a concentration of 5 nM. Monomethyl auristatin E (MMAE, 5 nM) and ionizing radiation (IR) treated cells are harvested and lysed in RIPA buffer with protease and phosphatase inhibitors. 30 μg of lysate undergo electrophoresis using 4-12% Bis-Tris gels, transferred to PVDF membranes and incubated with indicated primary antibodies.

6-8 week old female athymic nu/nu mice are injected subcutaneously into thighs with 5×106 HCT-116 or PANC-1 cells in a 1:1 Matrigel and PBS solution. Mice are treated with IR or intravenous (IV) injection of ACPP-cRGD-MMAE (6 nmoles/day, 18 nmoles total, i.v.), tumor tissue is harvested, formalin fixed and paraffin embedded followed by staining with indicated antibodies. The primary antibody is used at a 1:250 dilution and is visualized using DAB as a chromagen with the UltraMap system.