MT-DADMe-ImmA (MTDIA) is an inhibitor of human 5'-methylthioadenosine phosphorylase (MTAP, Ki: 90 pM).

MTAP:90 pM (Ki, cell free)

在培养细胞中使用MTA和MT-DADMe-ImmA可抑制MTAP活性，增加细胞内MTA浓度，降低多胺水平，并在两种头颈部鳞状细胞癌细胞系FaDu和Cal27中诱导凋亡。单独使用MT-DADMe-ImmA并不在任何细胞系中诱发凋亡[2]。

MTAP 活性逐渐恢复，口服 MT-DADMe-ImmA 的生物半衰期为 6.3 天。在免疫缺陷鼠中，FaDu 肿瘤的时间依赖性增长通过口服或腹腔内使用 MT-DADMe-ImmA [2] 被抑制。

Cell viability is evaluated using the Alamar Blue assay. Cells are seeded onto 96-well plates at a density of 10^4 cells/well and incubated with increasing concentrations of MT-DADMe-ImmA (100 pM to 100 μM) for 4 days at fixed MTA concentrations (0, 5, 10, and 20 μM) [2].

Tumors were established in mice for 5 days prior to oral or intraperitoneal treatments with MT-DADMe-ImmA. Mice are treated with an oral dose of 21 mg/kg or an intraperitoneal dose of 5 mg/kg/day MT-DADMe-ImmA [2].