Talabostat (mesylate)

一种非选择性DPP抑制剂（DPP-4、DPP-7、DPP-8、DPP-9、FAP和PREP的IC50分别为>4、310、4、11、560和390nM）；抑制超抗原刺激的人PBMCs增殖（IC50=~10nM）；每天两次5μg剂量可增加WEHI-164纤维肉瘤小鼠模型中肿瘤和肿瘤引流淋巴结中多种细胞因子和趋化因子的表达；降低多种同系小鼠模型中的肿瘤生长；分别增强抗肿瘤抗体利妥昔单抗和曲妥珠单抗在NamalwaB细胞淋巴瘤和LS180结肠癌小鼠异种移植模型中的疗效。A non-selective inhibitor of DPPs (IC50s = >4, 310, 4, 11, 560, and 390 nM for DPP-4, DPP-7, DPP-8, DPP-9, FAP, and PREP, respectively); inhibits proliferation of superantigen-stimulated human PBMCs (IC50 = ~10 nM); increases expression of a variety of cytokines and chemokines in tumors and tumor-draining lymph nodes in a WEHI-164 fibrosarcoma mouse model at 5 μg twice per day; reduces tumor growth in a variety of syngeneic mouse models; increases the efficacy of the antitumor antibodies rituximab and trastuzumab in Namalwa B cell lymphoma and LS180 colon carcinoma mouse xenograft models, respectively.