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编 号:F748393
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1mg
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5mg
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生物活性:
Dostarlimab (TSR-042) is a humanized anti-PD-1 monoclonal antibody. Dostarlimab binds with high affinity to human PD-1 and competitively inhibits its interaction with its ligands, PD-L1 and PD-L2, with IC50s of 1.8 and 1.5 nM, respectively.

体内研究:
Dostarlimab (200 μg/mouse; i.p.; twice weekly for 35 days) 在人源化小鼠模型中显示出抗肿瘤活性。Animal Model:Humanized NOG-EXL mice, A549 and MDA-MB-436 tumor model
Dosage:200 μg/mouse
Administration:Intraperitoneal injection; twice weekly for 35 days
Result:Resulted in great inhibition of tumor growth in an A549 lung cancer model (tumor growth inhibition [TGI] of 62% at termination). The antitumor activity was associated with a reduction in tumor-associated regulatory T cells and a trend toward increased tumor-infiltrating CD8+ T cells. Inhibited tumor growth of MDA-MB-436 breast cancer model (TGI of 53%).

体外研究:
Dostarlimab (10-10000 ng/mL) 以剂量依赖的方式与人和食蟹猴 CD3+ T 细胞上表达的原生 PD-1 受体结合。Dostarlimab (0-375 nM; 48 h) 在人 CD4+ T 细胞 MLR 实验中增加 IL-2 的产生,EC50 大约为 1 nM,在葡萄球菌肠毒素 B (SEB) 刺激的 PBMC 细胞中增加 IL-2 的产生,EC50 大约为 0.1 nM,增强干扰素 (IFN)-γ 的释放,EC50 大约为 0.5 nM。
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